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TAK-285

Chemical Structure : TAK-285

CAS No.: 871026-44-7

TAK-285 (TAK285)

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
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 547.96
分子式 C26H25ClF3N5O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

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

参考文献

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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