TYRA-200 represents a next-generation covalent inhibitor specifically engineered to target FGFR2, addressing critical limitations in current therapeutic options. The fibroblast growth factor receptor 2 plays pivotal roles in cellular proliferation and differentiation, with its genetic alterations strongly implicated in intrahepatic cholangiocarcinoma (iCCA) pathogenesis - particularly the FGFR2 fusions observed in 10-15% of iCCA cases. While pan-FGFR inhibitors have recently emerged as treatment options for advanced biliary tract cancers, their clinical utility is frequently compromised by polyclonal resistance mutations, predominantly within the FGFR2 kinase domain. TYRA-200 was developed through structure-guided rational design to overcome these resistance mechanisms.
Cat.No
DC67580
Name
TYRA-200
Chemical Properties
CAS
Formula
MW
Storage
2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
References
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