Search Result
Results for "
Ba/F3
" in MedChemExpress (MCE) Product Catalog:
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-164397
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Anaplastic lymphoma kinase (ALK)
Apoptosis
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Cancer
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XMU-MP-5 is a selective inhibitor for ALK. XMU-MP-5 inhibits ALK-mutated Ba/F3 cell with IC50s of 4-50 nM, and induces apoptosis in EML4-ALK Ba/F3. XMU-MP-5 exhibits antitumor efficacy in mice .
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- HY-18960
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CHZ868
5 Publications Verification
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JAK
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Cancer
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CHZ868 is a type II JAK2 inhibitor with an IC50 of 0.17 μM in EPOR JAK2 WT Ba/F3 cell.
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- HY-104010
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Asciminib
Maximum Cited Publications
9 Publications Verification
ABL001
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Bcr-Abl
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Cancer
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Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-12083
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Bcr-Abl
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Cancer
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PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba?F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML) .
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- HY-163366
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Trk Receptor
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Cancer
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TRK-IN-28 (compound 30f) is a TRK inhibitor with the IC50 values of 0.55 nM, 25.1 nM and 5.4 nM against TRK WT, TRK G595R and TRK G667C, respectively. TRK-IN-2 shows antiproliferative activity with IC50 values of 9.5, 3.7, 205.0 and 48.3 nM against Ba/F3-ETV6-TRKA WT, Ba/F3-ETV6-TRKB WT, Ba/F3-LMNA-TRK G595R and Ba/F3-LMNA-TRKA G667C, respectively .
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- HY-170928
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EGFR
Anaplastic lymphoma kinase (ALK)
Cytochrome P450
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Cancer
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DA-0157 is the orally active inhibitor for EGFR and ALK that overcomes drug-resistant mutations of EGFR C797S and ALK in NSCLC) cells. DA-0157 inhibits the proliferation of Ba/F3-EGFR Del19/T790M/C797S (IC50 = 6.9 nM), Ba/F3-EGFR WT (IC50 = 0.83 μM), Ba/F3-EML4-ALK-L1196M (IC50 = 5.5 nM), and Ba/F3-EML4-ALK (IC50 = 7.4 nM). DA-0157 inhibits CYP2D6 with IC50 of 5.26 μM. DA-0157 exhibits antitumor efficacy in mouse models .
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- HY-162881
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EGFR
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Cancer
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DS06652923 is an orally active EGFR triple mutation inhibitor. DS06652923 has a growth inhibition effect on Ba/F3 EGFR del19/T90M/C797S cells, with a GI50 value of 9.4 nM. DS06652923 can lead to tumor regression in Ba/F3 xenograft models .
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- HY-126920
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FLT3
Apoptosis
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Cancer
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AFG206 is a first-generation ATP competitive “type II” FLT3 inhibitor. AFG206 potently inhibits cell proliferation (IC50 around 0.1 µM) via induction of Apoptosis in FLT3-ITD-Ba/F3 cells and D835Y-Ba/F3 cells. AFG206 is promising for research of acute myeloid leukemia .
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- HY-174330A
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Trk Receptor
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Cancer
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TRK-IN-31 hydrochloride is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 hydrochloride has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 hydrochloride significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
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- HY-174330
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Trk Receptor
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Cancer
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TRK-IN-31 is an orally active TRK inhibitor with an IC50 of 1.8 nM. TRK-IN-31 has superior antiproliferative activity in the Ba/F3-MPRIP-TRKA G667C cells, and potently inhibits TRK kinase activity with high selectivity. TRK-IN-31 significantly inhibits tumor growth in Ba/F3-MPRIP-TRKA G667C subcutaneous tumor mice model .
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- HY-104010A
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ABL001 hydrochloride
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Bcr-Abl
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Cancer
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Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-149965
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Trk Receptor
Apoptosis
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Cancer
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TRK-IN-23 (compound 24b) is a potent and orally active TRK inhibitor with IC50 values of 0.5 nM, 9 nM, 14 nM, 4.4 nM, and 4.8 nM against TRKA, TRKC, TRKA G595R, TRKA F589L, and TRKA G667C, respectively. TRK-IN-23 indues apoptosis of Ba/F3-TRKAG595Rand Ba/F3-TRKAG667C cells .
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- HY-163004
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Trk Receptor
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Cancer
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Type II TRK inhibitor 2 (compound 40l) is a selective type II TRK inhibitor with plasma stability and moderate hepatic microsomal stability. Type II TRK inhibitor 2 significantly inhibits Km-12, Ba/F3-TRKA G595R and Ba/F3-TRKA G667C cell proliferation (IC50: 4.1 nM, 41.5 nM, 1.4 nM). Type II TRK inhibitor 2 can be used to study NTRK fusion cancers .
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- HY-159642
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FGFR
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Cancer
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TYRA-300 is an orally active, selective inhibitor for FGFR3 with an IC50 of 11 nM in Ba/F3. TYRA-300 exhibits antitumor efficacy against urothelial cancers and solid tumors .
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- HY-11007
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GNF-2
2 Publications Verification
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Bcr-Abl
SARS-CoV
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Cancer
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GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
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- HY-18952A
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FLT3
Apoptosis
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Cancer
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(Z)-SU5614 is a potent FLT3 inhibitor and selectively induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3 .
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- HY-110026
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FLT3
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Cancer
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GTP-14564 is a tyrosine kinase inhibitor targeting to internal tandem duplication (ITD) and FLT3. GTP-14564 inhibits FLT3 ligand-dependent growth in Ba/F3 leukemia cells .
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- HY-104010R
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ABL001 (Standard)
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Reference Standards
Bcr-Abl
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Cancer
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Asciminib (Standard) is the analytical standard of Asciminib. This product is intended for research and analytical applications. Asciminib (ABL001) is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM .
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- HY-144451
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Trk Receptor
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Cancer
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TRK-IN-12 (Compound 9e) is a potent inhibitor of TRK (TRK G595R IC50 = 13.1 nM). TRK-IN-12 is a macrocyclic derivative compound. TRK-IN-12 shows significant antiproliferative activity in the Ba/F3-LMNA-NTRK1 cell line (IC50 = 0.080 μM). TRK-IN-12 has shown a better inhibitory effect (IC50 = 0.646 μM) than control agent LOXO-101 in Ba/F3-LMNA-NTRK1-G595R cell line .
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- HY-170927
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JAK
STAT
Apoptosis
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Cancer
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JAK-IN-40 (Compound 46) is the inhibitor for JAK that inhibits JAK1, JAK2 and JAK3 with IC50s of 0.022, 0.759 and 1.601 μM, respectively. JAK-IN-40 inhibits the phosphorylation of STAT3. JAK-IN-40 inhibits the proliferation of cancer cell Ba/F3 and JAK1-TEL Ba/F3 with GI50 of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle of H1975 and H2087 at G2/M phase, induces apoptosis. JAK-IN-40 exhibits a synergistic antitumor effect with Osimertinib (HY-15772) .
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- HY-12291
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HMSL 10017-101-1
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Raf
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Cancer
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HG6-64-1 is a potent and selective B-Raf inhibitor extracted from patent WO 2011090738 A2, example 9 (XI-1); has a IC50 of 0.09 μM on B-raf V600E transformed Ba/F3 cells.
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- HY-13491
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Trk Receptor
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Cancer
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GNF-5837 is a potent, selective, and orally bioavailable pan-tropomyosin receptor kinase (TRK) inhibitor which display antiproliferative effects in cellular Ba/F3 assays ( IC50 values of 7 nM, 9 nM and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively) .
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- HY-174415
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PROTACs
EGFR
Akt
ERK
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Cancer
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ZSH-2117 is a covalent and selective EGFR PROTAC degrader with a DC50 of 45 nM in Ba/F3-EGFR L858R/T790M/C797S cells. ZSH-2117 significantly inhibits cell proliferation and reduces the downstream EGFR signaling proteins level of AKT and ERK. ZSH-2117 effectively inhibits tumor growth in Ba/F3-EGFR L858R/T790M/C797S xenograft mice model . Pink: EGFR ligand (HY-175162); Blue: NEDD4 ligase ligand (HY-175159); Black: linker
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- HY-157432
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EGFR
Apoptosis
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Cancer
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EGFR-IN-97 (compound 6q) is a EGFR inhibitor. EGFR-IN-97 shows inhibitory activity against Ba/F3-EGFR L858R/T790M/C797S and Ba/F3-EGFR Del19/T790M/C797S cells, with IC50 values of 0.42 μM and 0.41 μM, respectively. EGFR-IN-97 can promote apoptosis of NCI-H1975-EGFR L858R/T790M/C797S cells at the concentration of 0.8 μM .
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- HY-142922
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Bcr-Abl
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Cancer
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BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11) .
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- HY-11007R
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Bcr-Abl
SARS-CoV
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Cancer
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GNF-2 (Standard) is the analytical standard of GNF-2. This product is intended for research and analytical applications. GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
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- HY-112378
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FLT3
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Cancer
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D-65476 is an inhibitor of type Ⅲ receptor tyrosine kinase (Flt3). In the absence of IL-3, D-65476 inhibits the proliferation of TEL-Flt3 transfected BA/F3 cells (IC50= 0.2 μM), which can be used in the study of Flt3-driven leukemia .
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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-131244
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Anaplastic lymphoma kinase (ALK)
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Cancer
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ALK-IN-9 (compound 40) is a potent ALK inhibitor. ALK-IN-9 inhibits cell proliferation with IC50s of <0.2 nM, <0.2 nM, 0.2 nM for Ba/F3-EML4-ALK, KM 12 (TPM3-TRKA), KG-l cell (OP2-FGFR1), respectively .
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- HY-159147
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PROTACs
ROS Kinase
Apoptosis
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Cancer
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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- HY-170497
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EGFR
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Cancer
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EGFR-IN-140 (Compound 31) is the inhibitor for EGFR, that inhibits EGFR wildtype and EGFR L858R/T790M/C797S mutant with Ki of 0.95 nM and 2.1 nM, and inhibits EGFR del19/T790M/C797S in Ba/F3 with an IC50 of 56.9 nM. EGFR-IN-140 exhibits antitumor efficacy in mouse model .
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- HY-151048
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EGFR
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Cancer
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JBJ-07-149 is an inhibitor for EGFRL858R/T790M with an IC50 of 1.1 nM. JBJ-07-149 inhibits the proliferation of cell Ba/F3 with IC50 of 4.9 μM and 0.148 μM, without and with presence of Cetuximab (HY-P9905). JBJ-07-149 can be used as ligand for target protein in synthesis of DDC-01-163 (HY-139997) .
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- HY-162645
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TAM Receptor
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Inflammation/Immunology
Cancer
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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 .
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- HY-125845
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VH032-NH2; VHL ligand 1
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-101763B
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VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) dihydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC dihydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-131906
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JAK
FLT3
Apoptosis
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Cancer
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3 V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities .
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- HY-133551
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RET
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Cancer
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WF-47-JS03 is a potent and selective RET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR). Effective brain penetration .
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- HY-126619
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Bacterial
Apoptosis
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Infection
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Aspochalasin D is a co-metabolite originally isolated from A. microcysticus with aspochalasins A, B, and C, that is initially thought to be inactive. It has antibacterial activity against Gram-positive and Gram-negative bacteria at a concentration of 1 mg/ml.2 Aspochalasin D is more cytotoxic, via apoptosis, to Ba/F3-V12 cells in an IL-3-free medium than in an IL-3-containing medium (IC50s=0.49 and 1.9 μg/mL, respectively).
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- HY-110402
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VH032-NH2 TFA; VHL ligand 1 TFA
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Ligands for E3 Ligase
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Cancer
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(S,R,S)-AHPC (VH032-NH2) TFA is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC TFA can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells .
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- HY-161269
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EGFR
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Cancer
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EGFR-IN-101 (I-10) is a 2-phenylamino pyrimidine derivative. EGFR-IN-101 is a EGFR inhibitor. The IC50 values for EGFR L858R/T790M/C797S and Ba/F3-EGFR L858R/T790M/C797S are 33.26 and 106.4 nM, respectively. EGFR-IN-101 can be used IN the study of non-small cell lung cancer (NSCLC) .
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- HY-155302
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FLT3
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Cancer
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FLT3-IN-22 (compound 22f) is a potent FLT3 inhibitor with IC50 values of 0.941 nM and 0.199 nM for FLT3 and FLT3/D835Y, respectively. FLT3-IN-22 exhibits strong antiproliferative activity against MV4-11 cells and the mutant FLT kinase expressed Ba/F3 cell lines, including FLT-D835Y and FLT3-F691L .
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- HY-125834
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PROTACs
Bcr-Abl
Apoptosis
STAT
JAK
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Cancer
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GMB-475 is a potent BCR-ABL1 PROTAC based on Von Hippel-Lindau (VHL). GMB-475 targets the nutmeg pocket of ABL1 in an ectopic manner and degrades BCR-ABL1 protein through the ubiquitin proteasome pathway. GMB-475 inhibits the proliferation of human K562 cells and mouse Ba/F3 cells, and is used for the study of chronic myeloid leukemia. (Blue: VHL ligand (HY-125845); Black: Linker; Pink: BCR-ABL1 ligand (HY-11007)) .
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- HY-146807
-
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Trk Receptor
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Cancer
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Type II TRK inhibitor 1 is a potent TRK inhibitor, which inhibits various TRK fusion protein variants and wild type. Type II TRK inhibitor 1 exhibits antiproliferative activity against Ba/F3 cells harboring CD74-TRKA G667C and ETV6-TRKC G696C fusion proteins with IC50s of 6 nM and 1.7 nM, respectively . Type II TRK inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-158313
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EGFR
PROTACs
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Cancer
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PROTAC EGFR degrader 13 (compound 106) is an EGFR PROTAC degrader with a DC50 of <0.1 μM. PROTAC EGFR degrader 13 has proliferation inhibitory activity on cell Ba/F3-TEL-EGFR-T790M-L858R-C797S with an IC50 of 15.6 nM. PROTAC EGFR degrader 13 can be used for the study of EGFR-related diseases such as cancer (Pink: Target protein ligand; Blue: E3 ligand (HY-14658); Black: linker (HY-W262798); E3 ligand + linker: HY-W998306) .
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- HY-156086
-
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Trk Receptor
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Cancer
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TRK-IN-24 (compound 10g) is a Trk Receptor inhibitor that inhibits TRKA, TRKC, TRKA G595R, TRKA G667C and TRKA F589L IC50s are 5.21, 4.51, 6.77, 1.42 and 6.13 nM respectively. TRK-IN-24 has antitumor efficacy in BaF3-CD74-NTRK1 G595R and BaF3-CD74-NTRK1 G667C xenograft models. TRK-IN-24 inhibits the proliferation of Ba/F3 cells transfected with single mutants such as SF, GK, and xDFG, with an IC50 of 1.43-47.56 nM .
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- HY-174981
-
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PROTACs
FGFR
ATP Synthase
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Cancer
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LC-MF-4 is a selective FGFR3 PROTAC degrader with a DC50 of 30.89 nM in KMS-11 cells. LC-MF-4 inhibits the metabolic function of FGFR3-TACC3 fusion positive cancers with reduction of ATP synthesis and inhibition of mitochondrial biogenesis genes. LC-MF-4 has potent antitumor activity in the Ba/F3-FGFR3-TACC3 xenograft mice model. LC-MF-4 can be used for FGFR3-altered cancers like bladder cancer and urothelial carcinoma (UC) research . Pink: FGFR3 ligand (HY-175414); Blue: VHL ligase ligand (HY-125905); Black: linker (HY-Y1224)
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- HY-170852
-
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PROTACs
RET
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Cancer
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QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .
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- HY-136526
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Bcr-Abl
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Cancer
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BCR-ABL-IN-3 is a potent and irreversible Bcr-Abl inhibitor with an IC50 of ≤100 nM for Ba/F3Bcr-Abl T3151. BCR-ABL-IN-3 has anti-cancer activity .
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Cat. No. |
Product Name |
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Classification |
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- HY-159147
-
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Azide
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SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) .
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