TAK 285

TAK-285是HER2和EGFR(HER1)抑制剂,IC50为17 nM和23 nM,比对HER4的抑制性高10倍以上,对MEK1/5,c-Met,Aurora B,Lck和CSK的抑制性较低。

研究领域 >> 癌症

EGFR:23 nM (IC50)

HER2:17 nM (IC50)

[1]. Ishikawa T, et al. Design and synthesis of novel human epidermal growth factor receptor 2 (HER2)/epidermal growth factor receptor (EGFR) dual inhibitors bearing a pyrrolo[3,2-d]pyrimidine scaffold. J Med Chem, 2011, 54(23), 8030-8050.

[2]. Aertgeerts K, et al. Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein. J Biol Chem, 2011, 286(21), 18756-18765.

[3]. Erdo F, et al. Verification of brain penetration of the unbound fraction of a novel HER2/EGFR dual kinase inhibitor (TAK-285) by microdialysis in rats. Brain Res Bull, 2012, 87(4-5), 413-419.

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