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TAK-285

CAS No. : 871026-44-7

MCE 国际站：TAK-285

产品活性：TAK-285 是一种有效的，选择性的，ATP 竞争性的且口服活性的 HER2 和 EGFR(HER1) 抑制剂，IC₅₀ 分别为 17 nM 和 23 nM。TAK-285 对 HER1/2 的选择性是 HER4 的 10 倍以上，对 MEK1/5，c-Met，Aurora B，Lck，CSK 等的效价较低。TAK-285 具有有效的抗肿瘤活性，可穿过血脑屏障。

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

作用靶点：EGFR

In Vitro: TAK-285 (Compound 34e) shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI₅₀ of 17 nM.TAK-285 (Compound 34e) exhibits HER4 inhibitory activity with an IC₅₀ value of 260 nM. TAK-285 also inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK and Lyn B with IC₅₀s of 1100 nM, 5700 nM, 4200 nM, 1700 nM, 2400 nM, 4700 nM and 5200 nM, respectively.

In Vivo: TAK-285 (Compound 34e; 50-100 mg/kg; oral administration; twice daily; for 14 days; female BALB/cAJcl mice) treatment exhibits dose-dependent tumor growth inhibition (tumor/control ratio [T/C]): 44% and 11% at 50 and 100 mg/kg, respectively) without significant body weight loss in mice.

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