产品
编 号:F193302
分子式:C19H15N3O6S
分子量:413.4
产品类型
结构图
CAS No: 1612888-66-0
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产品详情
生物活性:
Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity.
体内研究:
In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg,gavage, daily, 40 days, N=10) is well tolerated and results in potent antitumour activity.Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo. Animal Model:C57Bl/6 × DBA/2 F1 mice of 22–30 g
Dosage:10 mg/kg/d
Administration:Intraperitoneally, 0, 3 and 6 d
Result:Alofanib inhibits angiogenesis in mouse models.
体外研究:
Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in hFOB and SUM 52PE cells expressing different FGFR2 isoforms. Alofanib (0.2-0.8 μM, 6 hours) inhibits FGF-mediated proliferation in a panel of four cell lines representing several tumour types (triple-negative breast cancer, melanoma, and ovarian cancer) with GI50s of 16-370 nM.