| Name | TAK 960 hydrochloride |
|---|---|
| Supplier | Tocris Bioscience |
| Catalog | 4254 |
| Prices | $255.00, $1,045.00 |
| Sizes | 10 mg, 50 mg |
| Function Type | Inhibitor |
| Cas Number | 1137868-96-2 |
| 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)benzamidehydrochloride |
| Formula | C27H34F3N7O3.HCl |
| Molecular Weight | 598.06 |
| Purity | >98 % |
| Description | Potent PLK1 inhibitor (IC 50 values are 0.8, 16.9 and 50.2 nM for PLK1, PLK2 and PLK3 respectively). Exhibits >20-fold selectivity for PLK1 over FAK, MLCK and FES, and has minimal activity against a panel of 282 other kinases. Inhibits proliferation of a range of cancer cell lines in vitro and inhibits tumor growth of multiple human cancer cell xenografts in vivo . Orally bioavailable. |
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Hikichi Y, Honda K, Hikami K, Miyashita H, Kaieda I, Murai S, Uchiyama N, Hasegawa M, Kawamoto T, Sato T, Ichikawa T, Cao S, Nie Z, Zhang L, Yang J, Kuida K, Kupperman E. Mol Cancer Ther. 2012 Mar;11(3):700-9.
Nie Z, Feher V, Natala S, McBride C, Kiryanov A, Jones B, Lam B, Liu Y, Kaldor S, Stafford J, Hikami K, Uchiyama N, Kawamoto T, Hikichi Y, Matsumoto S, Amano N, Zhang L, Hosfield D, Skene R, Zou H, Cao X, Ichikawa T. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3662-6.