Chemical Structure : TAK-285
CAS No.: 871026-44-7
货号: PC-23313Not For Human Use, Lab Use Only.
TAK-285 is a potent, dual inhibitor of HER2 and EGFR (HER1) with IC50 of 17 nM and 23 nM, respectively.
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
5 mg | ¥1480 | In stock | |
10 mg | ¥2180 | In stock | |
25 mg | ¥3880 | In stock | |
50 mg | Get quote | ||
100 mg | Get quote |
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TAK-285 is a potent, dual inhibitor of HER2 and EGFR (HER1) with IC50 of 17 nM and 23 nM, respectively.
TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM.
TAK-285 (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.
分子量 | 547.96 | |
分子式 | C26H25ClF3N5O3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
N-(2-(4-((3-Chloro-4-(3-(trifluoromethyl)phenoxy)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-5-yl)ethyl)-3-hydroxy-3-methylbutanamide |
1. Aertgeerts K, et al. J Biol Chem. 2011 May 27;286(21):18756-65.
2. Ishikawa T, et al. J Med Chem. 2011 Dec 8;54(23):8030-50.
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