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FGFR4-IN-8

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, FGFR4^V550L, FGFR4^V550M and FGFR4^C552S 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.

Research Area：Cancer

Targets：FGFR

Related Small Molecules:Ferulic acid-13C3;FGFR-IN-7;PP58;FGFR3-IN-1;ENMD-2076 Tartrate;R1530;FGFR3-IN-3;Tyrosine kinase-IN-1;Heparan Sulfate;Futibatinib;SU4984;Roblitinib;PD173074;PF 477736;Lucitanib;Masitinib;Zoligratinib;FGFR4-IN-4;BLU9931;SM1-71;VSPPLTLGQLLS TFA;TG 100801;FGFR1 inhibitor-6

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