FGFR2-IN-3

Research use only, not for human use.

FGFR2-IN-3 is an orally active selective FGFR2 inhibitor.

Lirafugratinib (RLY-4008) is an orally active, irreversible and highly selective FGFR2 inhibitor with an IC50 of 3 nM. Lirafugratinib covalently binds to Cys491. Lirafugratinib targets FGFR2 primary alterations and resistance mutations and induces tumor regression while sparing other FGFRs.

Apoptosis AnalysisCell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:24 hResult:Induced dose-dependent cleavage of caspase-3 and poly (ADP-ribose) polymerase (PARP)-early markers of apoptosis.Apoptosis Analysis Cell Line:FGFR2-amplified gastric cancer cell line SNU-16 Concentration:IC50 (6 nM), IC90 Incubation Time:2 h Result:Demonstrated a dose-dependent reduction of phosphorylation of FGFR2 signaling pathway nodes, including FRS2, AKT, and ERK.

Animal Model:Female BALB/c nude mice with SNU-16 and AN3CA xenografts; female NOD SCID mice with CC13-7 and ICC13-7-FGFR2V564F xenografts Dosage:1, 3, 10, 30 mg/kg Administration:Orally; twice daily; for 15-30 days Result:Exhibited dose-dependent antitumor activity and induced tumor regression in all models.

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Angiogenesis

FGFR

FGFR

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2549174-42-5

509.53

C28H24FN7O2

>98% (HPLC)

In Vitro:?DMSO : 62.5 mg/mL (122.66 mM; Ultrasonic (<60°C)

CC(=C)C(=O)Nc1ccc(cc1)-c1c(-c2ccc(Oc3nccc(C)n3)c(F)c2)c2c(N)ncnc2n1C

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(-20℃)

With Ice Pack

≥ 2 years