Search Result
Results for "
FGFR-IN-1
" in MedChemExpress (MCE) Product Catalog:
9
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-145043
-
|
FGFR
|
Cancer
|
FGFR-IN-1 is a potent FGFR inhibitor with an IC50 of <100 nM for FGFR1, FGFR2, and FGFR3, respectively (patent US20130338134A1, example 219) [1].
|
-
-
- HY-12965
-
S49076
1 Publications Verification
|
FGFR
c-Met/HGFR
|
Cancer
|
S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
|
-
-
- HY-160124
-
|
FGFR
|
Cancer
|
Infigratinib-Boc is a derivative of Infigratinib containing a Boc (t-Butyloxy carbonyl) group. Infigratinib is an ATP-competitive pan-FGFR inhibitor .
|
-
-
- HY-15813
-
FGFR irreversible INhibitor-1
|
FGFR
|
Cancer
|
FIIN-1 is a potent, irreversible, selective FGFR inhibitor. FIIN-1 binds to FGFR1/2/3/4 and Flt1/4 with Kds of 2.8/6.9/5.4/120 nM and 32/120 nM respectively. The biochemical IC50s of FIIN-1 are 9.2, 6.2, 11.9, and 189 nM against FGFR1/2/3/4, respectively [1].
|
-
-
- HY-160013
-
|
FGFR
|
Cancer
|
FGFR-IN-12 (example 14), a pyrimidinyl aryl urea derivative, is a potent FGFR inhibitor .
|
-
-
- HY-168653
-
|
FGFR
|
Cancer
|
FGFR-IN-15 (compound 18i) is a pan-FGFR inhibitor with potently inhibitory activity against FGFR1-4. [1].
|
-
-
- HY-172921
-
|
FGFR
|
Cancer
|
FGFR-IN-18 (Compound KF7) is a lysine-targeting FGFR covalent inhibitor, with IC50s of: 1.1 nM for FGFR2, 1.3 nM for FGFR1, 31.5 nM for FGFR4. FGFR-IN-18 also has affinity for FGFR3 (inhibition rate of 52% at 10 nM). FGFR-IN-18 covalently modifies Lys485 (an reactive site of FGFRs) [1].
|
-
-
- HY-170846
-
|
FGFR
VEGFR
Bcr-Abl
FLT3
Cytochrome P450
|
Inflammation/Immunology
|
FGFRs-IN-1 (Compound A16) is the orally active inhibitor for FGFR, that inhibits FGFR1/2/3/4 with IC50s of 2.3, 7, 11, and 163 nM, respectively. FGFRs-IN-1 also inhibits VEGFR1/2/3, Abl, and Flt3 with IC50s of 61, 176, 112, 26, and 353 nM, respectively. FGFRs-IN-1 exhibits weak inhibitory efficacy against CYP enzymes. FGFRs-IN-1 reduces the expression of α-SMA and collagen I, and inhibits epithelial-mesenchymal transition (EMT) in TGF-β1 stimulated A549 cell. FGFRs-IN-1 exhibits anti-inflammatory activity in Bleomycin (HY-17565)-induced mouse pulmonary fibrosis model and CCl4 (HY-Y0298)-induced mouse liver fibrosis model [1].
|
-
-
- HY-12965A
-
|
FGFR
c-Met/HGFR
|
Cancer
|
S49076 hydrochloride is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.
|
-
-
- HY-164459
-
AZ12908010
|
FGFR
|
Cancer
|
AZ8010 (AZ12908010) is a potent FGFR1-3 inhibitor. AZ8010 has anti-proliferative activity and can be used for the research of cancer [1].
|
-
-
- HY-101544
-
|
FGFR
|
Cancer
|
ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner [1].
|
-
-
- HY-163705
-
|
PROTACs
FGFR
|
Cancer
|
BR-cpd7 is a PROTAC degrader for fibroblast growth factor receptor FGFR1/2 with DC50 of 10 nM. BR-cpd7 arrests cell cycle, inhibits proliferations of FGFR1/2 aberrant activated tumor cells. (Pink: ligand for target protein FGFR-IN-12 (HY-160013); Black: linker; Blue: ligand for E3 ligase Thalidomide-NH-CH2-COOH (HY-131717)) [1]
|
-
-
- HY-172923
-
|
FGFR
|
Cancer
|
Glu-IN-1 (compound AF1) is a covalent and selective FGFR2 inhibitor with an IC50 of 1.6 μM. Glu-IN-1 covalently modifies Glu489 in FGFR2 .
|
-
-
- HY-10981A
-
E7080 mesylate
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-10981
-
Lenvatinib
Maximum Cited Publications
60 Publications Verification
E7080
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-147621
-
|
FGFR
|
Cancer
|
FGFR-IN-6 (Compound 5) is a FGFR inhibitor . FGFR-IN-6 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-18708
-
JNJ-42756493
|
FGFR
Apoptosis
|
Cancer
|
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
|
-
-
- HY-10337
-
BMS-540215
|
VEGFR
Autophagy
|
Cancer
|
Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β [1].
|
-
-
- HY-148778
-
|
FGFR
|
Cancer
|
FGFR3-IN-4 is a selective FGFR3 inhibitor, with an IC50 value of less than 50 nM. FGFR3-IN-4 is at least 10 fold more selective for FGFR3 than for FGFR1 [1].
|
-
-
- HY-172618
-
|
FGFR
|
Cancer
|
FGFR1 inhibitor-18 (compound 16) is a potent FGFR1 inhibitor with an IC50 value of 1.31 nM. FGFR1 inhibitor-18 can occupy within the ATP-binding pocket of the target FGFR1 [1].
|
-
-
- HY-19981A
-
ARQ-087 Racemate
|
FGFR
|
Cancer
|
Derazantinib Racemate (ARQ-087 Racemate) is the racemate of Derazantinib. Derazantinib is an orally bioavailable, ATP competitive tyrosine kinase inhibitor; exhibits potent activity against FGFR1-3 chondrocytes with IC50s of 4.5, 1.8, and 4.5 nM, respectively.
|
-
-
- HY-10336
-
BMS-582664
|
VEGFR
Autophagy
|
Cancer
|
Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-10981S1
-
E7080-d5
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-101466A
-
|
FGFR
|
Cancer
|
E7090 succinate is an orally available, selective and potent inhibitor of FGFR1, FGFR2 and FGFR3 tyrosine kinase activities, with IC50 values of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/2/3/4, respectively [1].
|
-
-
- HY-10981S
-
E7080-d4
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-101466
-
|
FGFR
|
Cancer
|
E7090 is an orally available, potent, and selective FGFR inhibitor with IC50s of 0.71 nM, 0.50 nM, 1.2 nM, and 120 nM for FGFR1/FGFR2/FGFR3/FGFR4, respectively [1].
|
-
-
- HY-133980
-
|
Drug Metabolite
|
Cancer
|
O-Demethyl Lenvatinib is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-133980A
-
|
Drug Metabolite
|
Cancer
|
O-Demethyl Lenvatinib hydrochloride is a metabolite of Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET. Lenvatinib shows potent antitumor activities [1] .
|
-
-
- HY-10981R
-
|
VEGFR
FGFR
PDGFR
c-Kit
RET
|
Cancer
|
Lenvatinib (Standard) is the analytical standard of Lenvatinib. This product is intended for research and analytical applications. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-146541
-
|
FGFR
|
Cancer
|
FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3 .
|
-
-
- HY-10981AR
-
|
VEGFR
FGFR
PDGFR
RET
c-Kit
|
Cancer
|
Lenvatinib (mesylate) (Standard) is the analytical standard of Lenvatinib (mesylate). This product is intended for research and analytical applications. Lenvatinib mesylate (E7080 mesylate), an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-101768
-
PRN1371
1 Publications Verification
|
FGFR
c-Fms
|
Cancer
|
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively [1].
|
-
-
- HY-10337R
-
|
VEGFR
Autophagy
|
Cancer
|
Brivanib (Standard) is the analytical standard of Brivanib. This product is intended for research and analytical applications. Brivanib (BMS-540215) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM, and has moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β [1].
|
-
-
- HY-18708R
-
|
FGFR
Apoptosis
|
Cancer
|
Erdafitinib (Standard) is the analytical standard of Erdafitinib. This product is intended for research and analytical applications. Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
|
-
-
- HY-B0062
-
TKI258 lactate hydrate; CHIR-258 lactate hydrate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
-
- HY-10207
-
CHIR-258 lactate; TKI-258 lactate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
-
- HY-159503A
-
3D185; HH185
|
FGFR
c-Fms
|
Cancer
|
Segigratinib hydrochloride (3D185) is a potent inhibitor of FGFR1/2/3 and CSF-1R; The IC50 values for FGFR1, FGFR2, FGFR3 and CSF-1R are 0.5, 1.3, 3.6 and 3.8 nM, respectively. Segigratinib hydrochloride has antitumor activity [1].
|
-
-
- HY-10981S2
-
E7080-15N,d4
|
VEGFR
c-Kit
FGFR
RET
PDGFR
Isotope-Labeled Compounds
|
Cancer
|
Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
|
-
-
- HY-100019
-
BAY1163877
|
FGFR
|
Cancer
|
Rogaratinib (BAY1163877) is a potent and selective fibroblast growth factor receptor (FGFR) inhibitor. Rogaratinib inhibits FGFRs with IC50s of 11.2 nM (FGFR1), <1 nM (FGFR2), 18.5 nM (FGFR3), 127 nM (VEGFR3/FLT4), 201 nM (FGFR4), respectively [1] .
|
-
-
- HY-50904
-
BIBF 1120
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-11106
-
BIBF 1120 esylate
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-119367
-
|
FGFR
VEGFR
|
Cancer
|
ODM-203 is an orally active and selective FGFR/VEGFR inhibitor with IC50 values of 6, 11, 16, 5, 9, 26 and 35 nM for FGFR3/1/2 and VEGFR3/2/1/4, respectively. ODM-203 has strong anti-tumour activity and activates immune responses in the tumour microenvironment [1].
|
-
-
- HY-10336R
-
BMS-582664 (Standard)
|
VEGFR
Autophagy
|
Cancer
|
Brivanib (alaninate) (Standard) is the analytical standard of Brivanib (alaninate). This product is intended for research and analytical applications. Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-W758126
-
|
Isotope-Labeled Compounds
|
Others
|
(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
|
-
-
- HY-18817
-
|
Bcr-Abl
FGFR
Raf
RET
VEGFR
|
Cancer
|
AFG210 is a potent multi-target kinase inhibitor that primarily inhibits Abl kinase (IC50=330 nM), and also has inhibitory effects on other kinases such as B-Raf, C-Raf, FGFR-1, RET and VEGF receptors. AFG210 can be used to study chronic myeloid leukemia and other diseases with abnormal activation of Abl kinase [1].
|
-
-
- HY-158027
-
|
Raf
VEGFR
FGFR
|
Cancer
|
B-Raf IN 17 (Compound 8e) is a potent and orally active type II multi-kinase inhibitor. B-Raf IN 17 exhibits potent cellular-level suppression of BRAFWT, VEGFR-2, and FGFR-1 in A375 cell line, with IC50 values of 0.02, 0.18 and 1.65 μM, respectively. B-Raf IN 17 can be used for the research of cancer [1].
|
-
-
- HY-50904S2
-
BIBF 1120-d8
|
Isotope-Labeled Compounds
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-50904S
-
BIBF 1120-d3
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
-
- HY-10207R
-
CHIR-258 lactate (Standard); TKI-258 lactate (Standard)
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
Dovitinib (lactate) (Standard) is the analytical standard of Dovitinib (lactate). This product is intended for research and analytical applications. Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively [1].
|
-
-
- HY-50904R
-
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib (Standard) is the analytical standard of Nintedanib. This product is intended for research and analytical applications. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-50904S1
-
BIBF 1120-13C,d3
|
Isotope-Labeled Compounds
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-11106R
-
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib esylate (Standard) is the analytical standard of Nintedanib esylate. This product is intended for research and analytical applications. Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-50905S
-
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively [1] .
|
-
- HY-100491
-
|
FGFR
|
Cancer
|
H3B-6527 is an orally active, highly selective and covalent FGFR4 inhibitor with an IC50 of <1.2 nM. H3B-6527 has at least 250-fold selectivity over FGFR1-3 with IC50s of 320 nM, 1290 nM and 1060 nM respectively. H3B-6527 has potent anti-cancer activity [1].
|
-
- HY-150026
-
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity [1].
|
-
- HY-50905
-
CHIR-258; TKI258
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
c-Fms
|
Cancer
|
Dovitinib (CHIR-258) is an orally active, potent multi-targeted tyrosine kinase (RTK) inhibitor with IC50s of 1, 2, 36, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively. Dovitinib has potent antitumor activity [1] .
|
-
- HY-151903S
-
|
FGFR
|
Cancer
|
FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively [1].
|
-
- HY-165537
-
|
FGFR
Apoptosis
Bcl-2 Family
Caspase
TNF Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Siphonaxanthin is a keto-carotenoid with anti-angiogenic and anti-inflammatory activity, which is found in green algae. Siphonaxanthin upregulates the expression of death receptor 5 (DR5), induces cancer cell apoptosis, decreases the expression of Bcl-2, and activates caspase-3. Siphonaxanthin is also an inhibitor of FGFR-1. Siphonaxanthin inhibits the proliferation, migration, and tube formation of human umbilical vein endothelial cells (HUVECs), as well as the outgrowth of microvessels in the rat aortic ring. Siphonaxanthin is promising for research of diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis [1].
|
-
- HY-156632
-
KIN-3248
|
FGFR
|
Cancer
|
Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR1-4 that effectively inhibits wild-type and drug-resistant mutations (such as FGFR2 V565F, FGFR3 V555M). Resigratinib covalently binds to the Cys492 site of FGFR, blocks the FGFR signaling pathway, inhibits tumor cell proliferation and induces apoptosis. Resigratinib can be used for the study of FGFR2/3-driven solid tumors (such as cholangiocarcinoma and bladder cancer) [1] .
|
-
- HY-112345
-
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity [1].
|
-
- HY-170919
-
|
FGFR
|
Cancer
|
FGFR2/3-IN-2 (compound 10) is an orally active FGFR2 and FGFR3 inhibitor. FGFR2/3-IN-2 inhibits FGFR2 and FGFR3 with IC50s of 3.7 nM and 31.2 nM (preincubation time 1 h), respectively. FGFR2/3-IN-2 spares FGFR1/4 and other kinases without causing diarrhea and serum phosphate elevation in vivo. FGFR2/3-IN-2 induces tumor stasis or regression in the SNU-16 gastric cancer model [1].
|
-
- HY-145601
-
TT 00420
|
Aurora Kinase
FGFR
VEGFR
|
Cancer
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Tinengotinib (TT00420) is an orally active, spectrally selective small molecule kinase inhibitor targeting Aurora A/B (IC50=1.2-3.3 nM), FGFR1/2/3 (IC50=1.5-3.5 nM), VEGFRs, JAK1/2 and CSF1R. Tinengotinib blocks Aurora kinase-mediated cell cycle progression (inducing G2/M arrest), inhibits FGFR/JNK-JUN signaling pathway and activates MEK/ERK-dependent apoptotic pathway. Tinengotinib has the activity of anti-tumor proliferation, inducing apoptosis, inhibiting angiogenesis and regulating tumor microenvironment. Tinengotinib can be used in the study of triple-negative breast cancer (TNBC), gallbladder cancer and tumor immune microenvironment [1] .
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Chemical Structure |
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- HY-10981S
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Lenvatinib-d4 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
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- HY-50904S2
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Nintedanib-d8 is deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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- HY-50904S1
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Nintedanib- 13C,d3 is the 13C- and deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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- HY-10981S1
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Lenvatinib-d5 is the deuterium labeled Lenvatinib. Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
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- HY-10981S2
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Lenvatinib- 15N,d4 is 15N and deuterated labeled Lenvatinib (HY-10981). Lenvatinib (E7080) is an oral, multi-targeted tyrosine kinase inhibitor that inhibits VEGFR1-3, FGFR1-4, PDGFR, KIT, and RET, shows potent antitumor activities [1] .
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- HY-W758126
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(R)-Brivanib alaninate-d4 is the deuterium-labeled Brivanib (alaninate) (HY-10336). Brivanib alaninate (BMS-582664) is an ATP-competitive inhibitor against VEGFR2 with an IC50 of 25 nM; has moderate potency against VEGFR-1 and FGFR-1, but more than 240-fold against PDGFRβ [1].
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- HY-50904S
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Nintedanib-d3 is the deuterium labeled Nintedanib. Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
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- HY-50905S
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Dovitinib-d8 is the deuterium labeled Dovitinib. Dovitinib (CHIR-258) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/FGFR3, VEGFR1/VEGFR2/VEGFR3 and PDGFRα/PDGFRβ, respectively [1] .
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- HY-151903S
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FGFR2/3-IN-1 is a potent and selective FGFR2 and FGFR3 (FGFR) inhibitor with IC50s of 1 nM and 0.5 nM, respectively. FGFR2/3-IN-1 displays >40-fold selectivity over FGFR1/FGFR4 and other kinome. FGFR2/3-IN-1 also inhibits FGFR3 V555L and V555M mutants with IC50s of 2.7 nM and 6.1 nM, respectively [1].
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