In a FGFR-driven human tumour xenograft model, oral administration of alofanib (30 mg/kg) is well tolerated and resulted in potent antitumour activity[1]. Treatment with alofanib ablated experimental FGF-induced angiogenesis in vivo[1].
In Vitro
Alofanib inhibits phosphorylation of FRS2α with IC50s of 7 and 9 nM in cancer cells expressing different FGFR2 isoforms[1]. Alofanib (10-1000 nM) 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].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Tsimafeyeu I, et al. Targeting FGFR2 with alofanib (RPT835) shows potent activity in tumour models. Eur J Cancer. 2016 Jul;61:20-8.
[2]. Khochenkov DA, et al. Antiangiogenic Activity of Alofanib, an Allosteric Inhibitor of Fibroblast Growth Factor Receptor 2. Bull Exp Biol Med. 2015 Nov;160(1):84-7.
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