2765240-52-4
Chemical Structure
FGFR4-IN-8
- CAS No.: 2765240-52-4
- Formula:C32H34Cl2FN7O3
- Molecular Weight:654.56
IUPAC Name: (R)-N-(2-((5-(1-(3,5-dichloropyridin-4-yl)ethoxy)-1H-indazol-3-yl)amino)-3-fluoro-5-(4-morpholinopiperidin-1-yl)phenyl)acrylamide
InChIKey: NSQXUXMIWSHGRV-LJQANCHMSA-N
SMILES: C[C@@H](OC1=CC=C(C2=C1)NN=C2NC3=C(C=C(C=C3F)N4CCC(CC4)N5CCOCC5)NC(C=C)=O)C6=C(C=NC=C6Cl)Cl
Biological Activity: FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4V550L, FGFR4V550M and FGFR4C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model[1].
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FGFR4-IN-8 | FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4V550L, FGFR4V550M and FGFR4C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model. | |||||||||||||||||||||
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Keywords
