产品描述:
Derazantinib is a multi-kinase inhibitor.{46442} It is a pan inhibitor of FGF receptors (FGFRs; IC50s = 4.5, 1.8, 4.5, and 34 nM for FGFR1, -2, -3, and -4, respectively) and also inhibits 10 receptor tyrosine kinases, 8 non-receptor tyrosine kinases, and the calcium/calmodulin-dependent protein kinase QIK in a panel of 297 kinases (IC50s = 3-31 and 9.7 nM, respectively). Derazantinib decreases phosphorylation of FGFR in COS-1 cells expressing FGFR1, -2, -3, or -4 (IC50s = 10 µM, respectively) and inhibits the growth of 15 cancer cell lines with mutant, amplified, or translocated FGFR (GI50s = 0.1-1.7 µM). It reduces tumor growth and decreases tumor protein levels of phosphorylated FGFR, FGFR substrate 2 (FRS2), and ERK in a SNU-16 mouse xenograft model when administered at doses of 50 and 75 mg/kg.