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FGFR2 gatekeeper mutants

" in MedChemExpress (MCE) Product Catalog:
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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-175743

    FGFR Cancer
    TYRA-200 is a potent and orally active FGFR2 inhibitor. TYRA-200 inhibits the kinase activity of wild-type FGFR2 and its mutants. TYRA-200 induces significant tumor regression in FGFR2-driven cancer models. TYRA-200 can be used for the research of FGFR2-altered advanced solid tumors, intrahepatic cholangiocarcinoma, and endometrial cancer .
    TYRA-200
  • HY-178059

    FGFR p38 MAPK Akt ERK Apoptosis Cancer
    FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC50s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1 V561M and FGFR3 V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research .
    FGFR-IN-23
  • HY-162577

    FGFR Cancer
    FGFR-IN-14 (compound 10h) is a pan-FGFR inhibitor. FGFR-IN-14 inhibits FGFR1, FGFR2, FGFR3 and FGFR2 V564F gatekeeper mutant with IC50s of 46, 41, 99, and 62 nM, respectively. FGFR-IN-14 strongly suppresses NCI-H520 lung cancer cells, SNU-16 and KATO III gastric cancer cells proliferation with IC50s of 19, 59, and 73 nM, respectively .
    FGFR-IN-14

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