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Falnidamol

CAS No. : 196612-93-8

MCE 国际站：Falnidamol

产品活性：Falnidamol (BIBX 1382) 是一种具有口服活性的，选择性的 EGFR 酪氨酸激酶抑制剂，IC₅₀ 为3 nM。Falnidamol 对 ErbB2 (IC₅₀=3.4 μM) 和其他一系列相关酪氨酸激酶 (IC₅₀>10 μM) 的选择性 >1000倍。Falnidamol 是嘧啶-嘧啶化合物，具有抗癌活性。

研究领域：JAK/STAT Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：EGFR

In Vitro: Falnidamol (BIBX 1382) demonstrates antiproliferative activity in mitogenic assays performed with KB cells.

In Vivo: Falnidamol (BIBX 1382; p.o.; 10 mg/kg/day; 16 days) completely suppressed tumor growth of human A431 xenografts with respective a T/C value of 15% after 2 weeks of treatment.
Falnidamol (50 mg/kg/day for 2 weeks) results in dephosphorylation of the EGF receptor in A431 xenograft-bearing mice.
With Falnidamol (p.o.; 10 mg/kg/day; 16 days), the C_4h is 2222 nM and the C_24h is 244 nM.

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