- ARQ-087；ARQ087；ARQ 087；CPD1093
Derazantinib(ARQ-087) is an orally bioavailable inhibitor of the fibroblast growth factor receptor (FGFR) with IC50 values of 1.8 nM for FGFR2, and 4.5 nM for FGFR1 and 3, showing lower potency for FGFR4 (IC50=34 nM). It also inhibits RET, DDR2, PDGFRβ, VEGFR and KIT.
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
DMSO ：93 mg/mL (198.48 mM)
ARQ-087 has anti-proliferative activity in cell lines driven by FGFR dysregulation, including amplifications, fusions, and mutations. Cell cycle studies in cell lines with high levels of FGFR2 protein show a positive relationship between ARQ 087 induced G1 cell cycle arrest and subsequent induction of apoptosis. ARQ 087 inhibits the auto-phosphorylation of FGFR1 and FGFR2 in a dose-dependent manner. In Cos-1 cells overexpressing full-length FGFR1, FGFR2, FGFR3 and FGFR4, ARQ 087 inhibits their phosphorylation with EC50 values of < 0.123 μM, 0.185 μM, 0.463 μM, >10 μM respectively. ARQ 087 inhibits FGFR kinase by an ATP competitive mechanism, and is capable of inhibiting both the inactive and fully active forms of the FGFR kinase. Hence, ARQ 087 delays FGFR activation by inhibiting its autophosphorylation, as well as inhibition of the phosphorylated active kinase.
ARQ 087 attenuates FGFR signaling in SNU-16 human xenograft tumors, leading to a reduction in phospho-FGFR, phospho-FRS2-α, and phospho-ERK, while the total FGFR2 protein is unaffecte. ARQ 087 is effective at inhibiting tumor growth in vivo in FGFR2 altered, SNU-16 and NCI-H716, xenograft tumor models with gene amplifications and fusions. ARQ 087 demonstrated efficacy in multiple in vivo xenograft models, and was well tolerated at doses up to 75 mg/kg.
- 提示： 尊敬的客户您好，如果您对我们的产品有什么疑问或想要了解的，可以点击“我要提问”按钮填写您的疑问。