Search Result
Results for "
Axl inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
4
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-155310
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YAP
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Cancer
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AF-2112 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2.
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- HY-155309
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YAP
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Cancer
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LM-41 is a Flufenamic acid-derived TEAD inhibitor hat strongly reduce the expression of CTGF, Cyr61, Axl and NF2. LM-41 inhibits migration of human MDA-MB-231 breast cancer cells .
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- HY-144708
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TAM Receptor
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Cancer
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Axl-IN-4 (Compound 24) is an AXL kinase inhibitor with an IC50 of 28.8 μM .
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- HY-144706
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TAM Receptor
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Cancer
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Axl-IN-3 is a potent, selective and orally active AXL kinase inhibitor with an IC50 of 41.5 nM. Axl-IN-3 has lower inhibition of other kinases .
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- HY-149491
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TAM Receptor
HIF/HIF Prolyl-Hydroxylase
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Others
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Axl-IN-16 (Compound 4) is a Axl inhibitor. Axl-IN-16 inhibits Axl expression and inhibits the activity of HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 can be isolated from“fruiting liquid (FL)” of Hypholoma lateritium and Hericium erinaceus .
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- HY-164382
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TAM Receptor
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Cancer
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ER-851 is a selective AXL inhibitor with oral activity with IC50 of 100 nM. ER-851 has antitumor activity .
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- HY-N12041
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TAM Receptor
HIF/HIF Prolyl-Hydroxylase
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Cancer
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Axl-IN-16 is a dual inhibitor of Axl/HIF. Axl-IN-16 induces fruiting body formation of Flammulina velutipes. Axl-IN-16 inhibits hypoxia-inducible factor activity and receptor tyrosine kinase expression .
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- HY-152075
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TAM Receptor
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Cancer
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AXL-IN-14 is a potent and orally active AXL inhibitor with an IC50 value of 0.8 nM. AXL-IN-14 inhibits Gas6/AXL-mediated cell migration and invasion. AXL-IN-14 decreases the expression of p-AXL and p-AKT proteins. AXL-IN-14 shows anti-tumor activity .
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- HY-146596
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TAM Receptor
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Cancer
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Axl-IN-5 (compound 1) is a AXL inhibitor with an IC50 of 283 nM. Axl-IN-5 has anticancer effects .
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- HY-153441
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TAM Receptor
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Cancer
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AXL-IN-15 (cpd391) is a potent Axl inhibitor with both Ki and IC50 <1 nM. AXL-IN-15 can be used for research in cancer .
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- HY-170776
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PDGFR
VEGFR
FGFR
Apoptosis
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Cancer
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AXL/Angiokinase-IN-1 (compound 11b) is an AXL/triple angiokinase inhibitor, IC50=3.75 nM (AXL expression). AXL/Angiokinase-IN-1 inhibits epithelial-mesenchymal transition (EMT) in Bxpc-3, blocking lung cancer cell metastasis. AXL/Angiokinase-IN-1 also inhibits vascular and fibroblast functions, promoting apoptosis (apoptosis) in cancer cells and fibroblasts. AXL/Angiokinase-IN-1 features low toxicity and good metabolic stability .
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- HY-162085
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TAM Receptor
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Cancer
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Axl-IN-17 (compound 13c) is an orally active, selective AXL inhibitor with an IC50 value of 3.2 nM. Axl-IN-17 reveals antitumor efficacy .
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- HY-146615
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TAM Receptor
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Cancer
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Axl-IN-6 (compound 14) is an orally active and potent AXL inhibitor. Axl-IN-6 is well tolerated and significantly inhibits the tumor growth in MV-4-11 subcutaneous xenograft model .
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- HY-162103
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TAM Receptor
Apoptosis
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Cancer
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Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC50=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC50=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model .
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- HY-153012
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TAM Receptor
c-Fms
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Cancer
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Axl/Mer-IN-1 (Compound 1) is an Axl/Mer receptor tyrosine kinase (Axl/Mer RTK) and CSF1R inhibitor with Kds of <0.1 μM .
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- HY-147575
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TAM Receptor
c-Met/HGFR
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Cancer
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Axl-IN-8 (NO.1) is a potent AXL inhibitor, with an IC50 of <1 nM. Axl-IN-8 also inhibits c-MET, with an IC50 of 1-10 nM. Axl-IN-8 shows anti-proliferative activity against BaF3/TEL-AXL, MKN45, and EBC-1 cells, with IC50 values of <10, 226.6 and 120.3 nM, respectively .
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- HY-147576
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TAM Receptor
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Inflammation/Immunology
Cancer
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Axl-IN-9 (Example 10) is a potent AXL inhibitor, with an IC50 of 26 nM. Axl-IN-9 has excellent transmembrane properties. Axl-IN-9 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-9 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals .
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- HY-147577
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TAM Receptor
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Inflammation/Immunology
Cancer
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Axl-IN-10 (Example 1) is a potent AXL inhibitor, with an IC50 of 5 nM. Axl-IN-10 has excellent transmembrane properties.Axl-IN-10 exhibits excellent pharmacokinetic properties in an animal body. Axl-IN-10 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancer, or other diseases in mammals .
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- HY-P99161
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BGB149
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TAM Receptor
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Cancer
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Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
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- HY-147574
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TAM Receptor
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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Axl-IN-7 (Chemie 22) is a potent AXL inhibitor. Axl-IN-7 can be used for Axl-related diseases research, for example cancers (such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glial tumors), renal disease, immune system disorders, and cardiovascular disease .
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- HY-176204
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TAM Receptor
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Cancer
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Axl-IN-19 (Compound 68) is a selective AXL (a membrane-bound receptor tyrosine kinase) inhibitor (IC50: 5.3 nM; Cellular KD = 6.8 nM). Axl-IN-19 has favorable rat PK with low clearance and moderate bioavailability. Axl-IN-19 can be used for cancer research .
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- HY-170954
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Apoptosis
c-Met/HGFR
TAM Receptor
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Cancer
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C-Met/Axl-IN-1 (Compound 22a) is an orally active and selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. C-Met/Axl-IN-1 can inhibit proliferation, induce cell cycle arrest and apoptosis of tumor cells. C-Met/Axl-IN-1 has strong anti-tumor activity .
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- HY-151904
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TAM Receptor
FLT3
PDGFR
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Cancer
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AXL-IN-13 is a potent and orally active AXL inhibitor (IC50: 1.6 nM, Kd: 0.26 nM). AXL-IN-13 reverses TGF-β1-induced epithelial-mesenchymal transition (EMT), and inhibits cancer cell migration and invasion .
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- HY-12494
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- HY-153277
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- HY-147578
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TAM Receptor
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Infection
Inflammation/Immunology
Cancer
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Axl-IN-11 (Example 1) is a potent AXL inhibitor. Axl-IN-11 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals .
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- HY-147579
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TAM Receptor
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Infection
Inflammation/Immunology
Cancer
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Axl-IN-12 (Example 2) is a potent AXL inhibitor. Axl-IN-12 can be used for the research of proliferative diseases, autoimmune diseases, allergic diseases, inflammatory diseases, transplant rejection, cancers, viral infectious diseases or other diseases of mammals .
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- HY-15494S1
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Axl1717-d6; Picropodophyllotoxin-d6; PPP-d6
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Isotope-Labeled Compounds
IGF-1R
Apoptosis
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Endocrinology
Cancer
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Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
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- HY-12432A
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ASP2215 hemifumarate
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FLT3
TAM Receptor
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Cancer
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Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
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- HY-12432
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ASP2215
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FLT3
TAM Receptor
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Cancer
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Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
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- HY-162940
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TAM Receptor
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Inflammation/Immunology
Cancer
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MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
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- HY-150041
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TAM Receptor
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Cancer
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TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research .
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- HY-149092
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TAM Receptor
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Cancer
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Anticancer agent 109 (compound 6-15) is an inhibitor of the Gas6-Axl axis with anti-cancer activity. Anticancer agent 109 inhibits the expression of Gas6 and Axl, and the expression p-PI3K and p-AKT in cancer cells, leads to G1 phase arrest and promotes cancer cells apoptosis, and inhibits tumor growth significantly in nude mouse tumor bearing models .
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- HY-12432S1
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ASP2215-d8
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FLT3
TAM Receptor
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Cancer
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Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
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- HY-12432R
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FLT3
TAM Receptor
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Cancer
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Gilteritinib (Standard) is the analytical standard of Gilteritinib. This product is intended for research and analytical applications. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
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- HY-P99921
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HuMax-Axl-ADC
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Antibody-Drug Conjugates (ADCs)
TAM Receptor
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Cancer
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Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
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- HY-P99463
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AVB-500; AVB-S6-500
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TAM Receptor
PI3K
Akt
p38 MAPK
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Cancer
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Batiraxcept (AVB-500; AVB-S6-500) is a selective, soluble AXL receptor and GAS6 inhibitor that targets the GAS6-AXL signaling axis. Batiraxcept is orally inactive and does not cross the blood-brain barrier. Batiraxcept competitively binds to GAS6 ((KD <1 nM), preventing its interaction with the AXL receptor tyrosine kinase, thereby inhibiting downstream PI3K/AKT and MAPK signaling pathways, reducing tumor cell glycolysis, angiogenesis, and metastatic potential. Batiraxcept has demonstrated antitumor activity in preclinical models of endometrial, cholangiocarcinoma, and ovarian cancer by inhibiting tumor growth, invasion, and metastasis .
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- HY-12963
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TP-0903
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TAM Receptor
Apoptosis
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Cancer
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Dubermatinib (TP-0903) is a potent and selective Axl receptor tyrosine kinase inhibitor with an IC50 value of 27 nM.
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- HY-100509
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- HY-162406
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TAM Receptor
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Cancer
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UNC8969 (compound 43) is a MERTK/AXL dual inhibitor with IC50s of 1.1±0.8 nM for MERTK and 5.3 ± 2.7 nM for AXL. UNC8969 also exerts a T1/2 of 7.3 h with 5 mg/kg i.v. in mice .
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- HY-145622
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BA3011; CAB-Axl-ADC; CAB-anti-Axl-ADC
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TAM Receptor
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Cancer
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Mecbotamab vedotin (BA301) is an IgG1 antibody inhibitor of anti-(human tyrosine kinase receptor AXL) (human-Mus musculus monoclonal BA301 γ1-chain). Mecbotamab vedotin can be used to make immunoconjugates for Methods of Axl-expressing cancers research .
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- HY-100946
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RXDX-106
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TAM Receptor
c-Met/HGFR
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Cancer
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CEP-40783 is a potent, selective and orally available inhibitor of AXL and c-Met with IC50 values of 7 nM and 12 nM, respectively.
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- HY-132893
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TAM Receptor
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Cancer
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AZ14145845 is a highly selective type I1/2 dual Mer/Axl kinase inhibitor with in vivo efficacy.
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- HY-12965A
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FGFR
c-Met/HGFR
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Cancer
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S49076 hydrochloride is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
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- HY-12965
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S49076
1 Publications Verification
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FGFR
c-Met/HGFR
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Cancer
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S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
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- HY-152830
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Q702
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c-Fms
TAM Receptor
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Cancer
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Adrixetinib (Q702) is an Axl/Mer/CSF1R protein tyrosine kinase inhibitor with antineoplastic activity .
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- HY-15494
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Axl1717; Picropodophyllotoxin; PPP
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IGF-1R
Apoptosis
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Endocrinology
Cancer
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Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
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- HY-170668
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- HY-114166
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E1/E2/E3 Enzyme
TAM Receptor
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Cancer
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2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
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- HY-152830A
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Q702 TFA
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c-Fms
TAM Receptor
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Cancer
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Adrixetinib (Q702) TFA is a selective Axl/Mer/CSF1R protein tyrosine kinase inhibitor with antineoplastic activity .
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- HY-114358
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ONO-7475
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TAM Receptor
Trk Receptor
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Cancer
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Tamnorzatinib (ONO-7475) is a potent, selective, and orally active Axl/Mer inhibitor with IC50 values of 0.7 nM and 1.0 nM, respectively. Tamnorzatinib sensitizes AXL-overexpressing EGFR-mutant NSCLC cells to the EGFR-TKIs, suppresses the emergence and maintenance of tolerant cells. Tamnorzatinib combines with Osimertinib (HY-15772) provides a bright promise for the study of EGFR-mutated non-small cell lung cancer (NSCLC).
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- HY-15150
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Bemcentinib
Maximum Cited Publications
47 Publications Verification
R428; BGB324
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TAM Receptor
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Cancer
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Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
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- HY-15797
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UNC2250
2 Publications Verification
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TAM Receptor
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Cancer
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UNC2250 is a potent and selective Mer inhibitor with an IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
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- HY-173400
-
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TAM Receptor
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Cancer
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UNC8212 is a TAM kinase inhibitor. UNC8212 has potent inhibitory activity against MERTK and AXL (IC50: 1.5 nM and 1.3 nM, respectively), and also inhibits TYRO3 (IC50: 6.7 nM). UNC8212 mediates polypharmacological properties by targeting the structurally diverse "back pocket" region of the TAM kinase family. UNC8212 binds tightly to TAM kinases and potently inhibits MERTK and AXL phosphorylation. UNC8212 has anti-tumor effects and can be used in cancer immunotherapy and tumor cell targeting research .
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- HY-12964
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TAM Receptor
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Cancer
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SGI-7079 is a selective, ATP-competitive, orally active inhibitor of the receptor tyrosine kinase Axl. SGI-7079 blocks Axl-mediated signaling pathways such as NF-κB activation and MMP-9 expression, thereby inhibiting tumor cell proliferation, migration and invasion. SGI-7079 is mainly used in the research of malignant tumors such as inflammatory breast cancer and bladder cancer, as well as in combination with immunization (used in combination with PD-1 therapy)[1][2][3].
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- HY-104075
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TAM Receptor
VEGFR
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Cancer
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R916562 is an orally active and selective Axl/VEGF-R2 inhibitor with IC50s of 136 nM and 24 nM, respectively. R916562 has anti-angiogenesis and anti-metastasis .
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- HY-107145A
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TAM Receptor
VEGFR
c-Met/HGFR
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Cancer
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Ningetinib is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
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- HY-124502
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TAM Receptor
FLT3
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Cancer
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UNC4203 is a potent, orally available and highly selective MERTK inhibitor, with IC50s of 1.2 nM, 140 nM, 42 nM and 90 nM for MERTK, AXL, TYRO3 and FLT3, respectively .
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- HY-107145
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TAM Receptor
VEGFR
c-Met/HGFR
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Cancer
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Ningetinib Tosylate is a potent, orally bioavailable small molecule tyrosine kinase inhibitor (TKI) with IC50s of 6.7, 1.9 and <1.0 nM for c-Met, VEGFR2 and Axl, respectively.
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- HY-W400801
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G-749 hydrochloride
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TAM Receptor
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Cancer
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Denfivontinib (G-749) hydrochloride is an AXL inhibitor that has synergistic antitumor effects with the PD-1 inhibitor Pembrolizumab (HY-P9902). Denfivontinib can enhance the NOD-like receptor pathway, thereby promoting the formation of the NLRP3 inflammasome .
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- HY-147218
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c-Met/HGFR
TAM Receptor
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Cancer
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PF-07265807 is a potent TAM and c-Met kinase inhibitor with IC50 values of 6.1 nM, 13.2 nM and 21.6 nM for AXL, MER and TYRO3, respectively. PF-07265807 can be used for researching anticancer .
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- HY-12044
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XL184 S-malate; BMS-907351 S-malate
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VEGFR
Apoptosis
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Cancer
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Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
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- HY-114356
-
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c-Met/HGFR
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Cancer
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BPI-9016M is a potent, orally active, and selective dual c-Met and AXL tyrosine kinases inhibitor. BPI-9016M suppresses tumor cell growth, migration and invasion of lung adenocarcinoma .
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- HY-15150G
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R428 (GMP); BGB324 (GMP)
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TAM Receptor
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Cancer
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Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
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- HY-13016S1
-
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XL184-d4; BMS-907351-d4
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VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
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Cancer
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Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
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- HY-162012
-
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YAP
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Cancer
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HC-258 (compound 26) binds with the cysteine in TEAD’s PA pocket. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells .
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- HY-132200
-
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TAM Receptor
Anaplastic lymphoma kinase (ALK)
FLT3
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Cancer
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UNC5293 is a MERTK-selective and potent inhibitor (Ki=190 pM). UNC5293 inhibits MERTK (IC50=0.9 nM) and is more selective over Axl, Tyro3 and Flt3. UNC5293 exhibits excellent mouse PK properties and is used for bone marrow leukemia research .
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- HY-13016S
-
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XL184-d6; BMS-907351-d6
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VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
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Cancer
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Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
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- HY-15798
-
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VSV
TAM Receptor
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Cardiovascular Disease
|
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UNC2881 is an orally active and specific Mer kinase inhibitor, inhibits steady-state Mer kinase phosphorylation with an IC50 value of 22 nM. UNC2881 shows additional inhibition against Axl and Tyro with IC50s of 360 nM and 250 nM, respectively. UNC2881 potently inhibits collagen-induced platelet aggregation, can be used for pathologic thrombosis research .
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- HY-14721
-
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EMD-1214063
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c-Met/HGFR
Autophagy
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Cancer
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Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
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- HY-117596
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UNC569
1 Publications Verification
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TAM Receptor
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Cancer
|
|
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
|
-
- HY-125510
-
UNC2541
1 Publications Verification
|
TAM Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
UNC2541 is a potent and Mer tyrosine kinase (MerTK)-specific inhibitor, binds in the MerTK ATP pocket, with an IC50 of 4.4 nM, more selective over Axl, Tyro3 and Flt3. UNC2541 inhibits phosphorylated MerTK (pMerTK; EC50, 510 nM). UNC2541 abolishes the analgesic and anti-inflammatory effects of ozone in vivo and in vitro .
|
-
- HY-14721A
-
|
EMD-1214063 hydrochloride
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
|
-
- HY-114357A
-
|
|
TAM Receptor
c-Met/HGFR
Trk Receptor
|
Cancer
|
|
DS-1205b free base is a potent and selective inhibitor of AXL kinase, with an IC50 of 1.3 nM. DS-1205b free base also inhibits MER, MET, and TRKA, with IC50s of 63, 104, and 407 nM, respectively. DS-1205b free base can inhibit cell migration in vitro and tumor growth in vivo .
|
-
- HY-168704
-
|
|
YAP
TAM Receptor
Survivin
|
Cancer
|
|
YAP/TAZ-TEAD-IN-2 (Compound 51) is a YAP/TAZ-TEAD inhibitor that inhibits the interaction between YAP/TAZ and TEAD. YAP/TAZ-TEAD-IN-2 suppresses the transcriptional activity of TEAD, with an IC50 of 1.2 nM. YAP/TAZ-TEAD-IN-2 inhibits YAP/TAZ-TEAD target genes expression (Cyr61, CTGF, AXL and Survivin) and breast cancer cell proliferation .
|
-
- HY-124066
-
|
|
TAM Receptor
|
Cancer
|
|
RU-302 is a pan TAM inhibitor that blocks the interface between the TAM Ig1 ectodomain and the Gas6 Lg domain. RU-302 effectively blocks Gas6-inducible Axl receptor activation with a low micromolar IC50in cell assays, and suppresses lung cancer tumor growth .
|
-
- HY-100833R
-
|
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-12044R
-
|
|
VEGFR
Apoptosis
|
Cancer
|
|
Cabozantinib (S-malate) (Standard) is the analytical standard of Cabozantinib (S-malate). This product is intended for research and analytical applications. Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-12344
-
UNC2025
4 Publications Verification
|
FLT3
|
Cancer
|
|
UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-12344A
-
|
|
FLT3
|
Cancer
|
|
UNC2025 hydrochloride is a potent, ATP-competitive, and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia .
|
-
- HY-14721R
-
|
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
|
-
- HY-116000
-
|
Gumarontinib; SCC244
|
c-Met/HGFR
|
Cancer
|
|
Glumetinib (SCC244) is a highly selective, orally bioavailable, ATP-competitive c-Met inhibitor with an IC50 of 0.42 nM. Glumetinib has greater than 2400-fold selectivity for c-Met over those 312 kinases evaluated, including the c-Met family member RON and highly homologous kinases Axl, Mer, TyrO3. Antitumor activity .
|
-
- HY-138696
-
|
XL092
|
TAM Receptor
c-Met/HGFR
VEGFR
|
Cancer
|
|
Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research .
|
-
- HY-117548
-
UNC1062
1 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC1062 is a MERTK-selective tyrosine kinase inhibitor, reduces activation of MERTK-mediated downstream signaling, induces apoptosis in culture, reduces colony formation in soft agar, and inhibits invasion of melanoma cells. UNC1062 potently inhibits MERTK kinase activity (MERTK IC50=1.1 nM, Morrison Ki=0.33 nM) and exhibits specificity within the TAM family (TYRO3 IC50=60 nM, AXL IC50=85 nM) .
|
-
- HY-N3634
-
|
|
EGFR
TAM Receptor
Tie
|
Cancer
|
|
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
|
-
- HY-13016A
-
|
XL184 hydrochloride; BMS-907351 hydrochloride
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib hydrochloride is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035 and 1.3 nM, respectively. Cabozantinib hydrochloride displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib hydrochloride shows antiangiogenic activity. Cabozantinib hydrochloride disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-120387
-
|
|
ROS Kinase
Anaplastic lymphoma kinase (ALK)
TAM Receptor
c-Met/HGFR
|
Cancer
|
|
SMU-B is the orally active inhibitor for ALK (IC50<0.5 nM), c-ros oncogene 1 (ROS1), c-MET (IC50=1.87 nM) and AXL (IC50=28.9 nM). SMU-B inhibits the proliferation of MKN45, H1993 and H441 with IC50s of 0.02 μM, 1.58 μM and 2.82 μM, respectively. SMU-B exhibits antitumor efficacy in mouse models .
|
-
- HY-162645
-
|
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
|
-
- HY-12076
-
|
BMS 817378
|
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
BMS 777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases .
|
-
- HY-13016
-
|
XL184; BMS-907351
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-12965B
-
|
|
TAM Receptor
|
Cancer
|
|
(Z)-S49076 hydrochloride is an orally active inhibitor of MET and AXL that blocks the downstream signaling of these receptors both in vitro and in vivo, inhibiting the proliferation and migration of tumor cells and suppressing tumor growth in xenograft models. (Z)-S49076 hydrochloride is capable of overcoming the resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) due to MET amplification in Erlotinib (HY-50896)-resistant cell lines both in vitro and in vivo. (Z)-S49076 hydrochloride can be used for research in non-small cell lung cancer (NSCLC) .
|
-
- HY-147695
-
|
|
c-Met/HGFR
|
Cancer
|
|
c-Met-IN-12 (compound 4r) is an orally active, potent and selective type II c-Met kinase inhibitor, with an IC50 of 10.6 nM. c-Met-IN-12 displays high inhibitory effects (inhibition rate > 80% in 1 μM) against AXL, Mer and TYRO3 kinases. c-Met-IN-12 can be used a scaffold for further kinase selectivity enhancement. c-Met-IN-12 shows antitumor efficacy .
|
-
- HY-16961
-
|
MGCD516; MG-516
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
|
Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
- HY-16961A
-
|
MGCD516 malate; MG-516 malate
|
VEGFR
c-Kit
FLT3
Discoidin Domain Receptor
Trk Receptor
|
Inflammation/Immunology
Cancer
|
|
Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively . Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment .
|
-
- HY-13016R
-
|
|
VEGFR
c-Met/HGFR
c-Kit
TAM Receptor
FLT3
Apoptosis
|
Cancer
|
|
Cabozantinib (Standard) is the analytical standard of Cabozantinib. This product is intended for research and analytical applications. Cabozantinib is a potent and orally active inhibitor of VEGFR2 and MET, with IC50 values of 0.035, and 1.3 nM, respectively. Cabozantinib displays strong inhibition of KIT, RET, AXL, TIE2, and FLT3 (IC50=4.6, 5.2, 7, 14.3, and 11.3 nM, respectively). Cabozantinib shows antiangiogenic activity. Cabozantinib disrupts tumor vasculature and promotes tumor and endothelial cell apoptosis .
|
-
- HY-15514A
-
|
LY2801653 dihydrochloride
|
c-Met/HGFR
FLT3
ROS Kinase
Discoidin Domain Receptor
|
Cancer
|
|
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
|
-
- HY-15514
-
|
LY2801653
|
c-Met/HGFR
FLT3
ROS Kinase
Discoidin Domain Receptor
|
Cancer
|
|
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
Fluorescent Dye
|
|
Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
|
| Cat. No. |
Product Name |
Type |
-
- HY-15150G
-
|
R428 (GMP); BGB324 (GMP)
|
Biochemical Assay Reagents
|
|
Bemcentinib (R428) GMP is Bemcentinib (HY-15150) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy.Bemcentinib (R428) is a selective and orally active Axl inhibitor with an IC50 of 14 nM. Bemcentinib retards cancer cell migration and invasion. Bemcentinib exhibits >100-fold selectivity for Axl versus Abl and 50- and >100-fold selectivity over TAM family kinases Mer and Tyro3, respectively, in cells. Bemcentinib blocks tumor spread and prolongs survival in models of metastatic breast cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99161
-
|
BGB149
|
TAM Receptor
|
Cancer
|
|
Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
|
-
- HY-P99463
-
|
AVB-500; AVB-S6-500
|
TAM Receptor
PI3K
Akt
p38 MAPK
|
Cancer
|
|
Batiraxcept (AVB-500; AVB-S6-500) is a selective, soluble AXL receptor and GAS6 inhibitor that targets the GAS6-AXL signaling axis. Batiraxcept is orally inactive and does not cross the blood-brain barrier. Batiraxcept competitively binds to GAS6 ((KD <1 nM), preventing its interaction with the AXL receptor tyrosine kinase, thereby inhibiting downstream PI3K/AKT and MAPK signaling pathways, reducing tumor cell glycolysis, angiogenesis, and metastatic potential. Batiraxcept has demonstrated antitumor activity in preclinical models of endometrial, cholangiocarcinoma, and ovarian cancer by inhibiting tumor growth, invasion, and metastasis .
|
-
- HY-P99921
-
|
HuMax-Axl-ADC
|
Antibody-Drug Conjugates (ADCs)
TAM Receptor
|
Cancer
|
|
Enapotamab vedotin is an AXL-targeted antibody-drug conjugate (ADC) with inhibitory potential against high AXL expressing non-small cell lung cancer (NSCLC). Enapotamab vedotin also exhibits resistant to EGFR inhibitor such as Osimertinib (HY-15772) .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-15494
-
-
-
- HY-N12041
-
-
-
- HY-N3634
-
|
|
Structural Classification
Leguminosae
Source classification
Phenols
Polyphenols
Psoralea corylifolia L.
Plants
|
EGFR
TAM Receptor
Tie
|
|
Corylifol C is a potent protein kinase inhibitor with IC50 valueS of 8.7, 3.0, 2.1, 6.4, 4.5, 6.2, 2.3, 1.2, 5.1 μg/ml for ARK5, Aurora-A, Aurora-B, AXL, B-RAF-VE, CDK4/CycD1, TIE2, EGF-R, EPHB4, respectively .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-12432S1
-
|
|
|
Gilteritinib-d8 is deuterium labeled Gilteritinib. Gilteritinib (ASP2215) is a potent and ATP-competitive FLT3/AXL inhibitor with IC50s of 0.29 nM/0.73 nM, respectively.
|
-
-
- HY-13016S
-
|
|
|
Cabozantinib-d6 is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively .
|
-
-
- HY-15494S1
-
|
|
|
Picropodophyllin-d6 (AXL1717-d6) is deuterium labeled Picropodophyllin. Picropodophyllin (AXL1717) is a selective insulin-like growth factor-1 receptor (IGF-1R) inhibitor with an IC50 of 1 nM.
|
-
-
- HY-13016S1
-
|
|
|
Cabozantinib-d4 is deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
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