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Alofanib

CAS No. : 1612888-66-0

MCE 站：Alofanib

产品活性：Alofanib (RPT835)是高效和选择性的成纤维细胞生长因子受体2 (FGFR2) 的变构抑制剂。抗癌活性。抗血管生成活性。

研究领域：Protein Tyrosine Kinase/RTK  |  Apoptosis

作用靶点：FGFR  |  Apoptosis

In Vitro: 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.

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.

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

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