Alofanib

Cat. No. :	HY-17601
M.Wt:	413.40
Formula:	C19H15N3O6S
Purity:	>98 %
Solubility:	DMSO : ≥ 30.1 mg/mL

Introduction of 1612888-66-0 :

Alofanib (RPT835) is a potent and selective allosteric inhibitor of fibroblast growth factor receptor 2 (FGFR2). Anticancer and antiangiogenic activity^[1][2]. IC50 & Target: FGFR2^[1] In Vitro: Alofanib inhibits phosphorylation of FRS2α with IC₅₀s of 7 and 9 nM in hFOB and SUM 52PE cells expressing different FGFR2 isoforms^[1].

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^[1].

In Vivo: 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^[1].

Treatment with alofanib (10 mg/kg/d, 0, 3 and 6 d, intraperitoneally) ablates experimental FGF-induced angiogenesis in vivo^[1].