Resigratinib (KIN-3248) is an irreversible and orally active covalent inhibitor of FGFR 1-4 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 ).
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