B-Raf inhibitor 是一种有效的双重 TGFβ-activated kinase 1 (TAK1) 和 mitogen-activated protein kinase kinase kinase 2 (MAP4K2) 抑制剂,IC50 分别为 41.1 nM 和 18.2 nM。
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TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
TAK1/MAP4K2 inhibitor 1 has moderate terminal elimination half-life (t1/2=2.94 h for mice (1 mg/kg, iv))[1].
参考文献:
[1]. Tan L, et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96.
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