TAK-960
Cat. No.：YN290332
CAS No. ：1137868-52-0
| 产品名称: | TAK-960 |
| CAS No.: | 1137868-52-0 |
| Chemical Name: | 4-[(9-cyclopentyl-7,7-difluoro-6,7,8,9-tetrahydro-5-methyl-6-oxo-5H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methyl-4-piperidinyl)-benzamide |
| Synonyms: | TAK 960,TAK960 |
| 分子量: | 561.60 |
| 分子式: | C₂₇H₃₄F₃N₇O₃ |
| SMILES: | O=C(NC1CCN(C)CC1)C2=CC(OC)=C(NC3=NC=C(N4C)C(N(C5CCCC5)CC(F)(F)C4=O)=N3)C=C2F |
| 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-960 是一种有效的，可口服的，选择性的polo-like kinase 1 (PLK1)抑制剂，IC50为 0.8 nM。TAK-960 对 PLK2 和 PLK3 也有抑制作用，IC50分别为 16.9 和 50.2 nM。TAK-960 抑制多种肿瘤细胞系的增殖，对多种肿瘤异种移植具有显著的疗效。 |
| IC50和靶点: | [{name:"PLK1:0.8 nM (IC50)"},{name: "PLK2:16.9 nM (IC50)"},{name: "PLK3:50.2 nM (IC50)"},{name: "FAK/PTK2:19.6 nM (IC50)"},{name: "MLCK/MYLK:25.6 nM (IC50)"},{name: "FES/FPS:58.2 nM (IC50)"}] |
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Hikichi, Y., Honda, K., Hikami, K., et al.TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimensMol. Cancer Ther.11(3),700-709(2012)
Nie, Z., Feher, V., Natala, S., et al.Discovery of TAK-960: An orally available small molecule inhibitor of polo-like kinase 1 (PLK1)Bioorg. Med. Chem. Lett.23(12),3662-3666(2013)
