TAK-285
Cat. No.:YN340167
CAS No. :871026-44-7
产品名称: | TAK-285 |
CAS No.: | 871026-44-7 |
Chemical Name: | N-[2-[4-[[3-chloro-4-[3-(trifluoromethyl)phenoxy]phenyl]amino]-5H-pyrrolo[3,2-d]pyrimidin-5-yl]ethyl]-3-hydroxy-3-methyl-butanamide |
Synonyms: | TAK 285,TAK285 |
分子量: | 547.96 |
分子式: | C₂₆H₂₅ClF₃N₅O₃ |
SMILES: | ClC(C=C(NC1=NC=NC2=C1N(CCNC(CC(C)(C)O)=O)C=C2)C=C3)=C3OC4=CC=CC(C(F)(F)F)=C4 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | 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。 |
IC50和靶点: | [{name:"EGFR:23 nM (IC50)"},{name: "HER2:17 nM (IC50)"}] |
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Ishikawa, T., Seto, M., Banno, H., 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 scaffoldJ. Med. Chem.54(23),8030-8050(2011)