货号 | 4786/50 |
别名 | 6-acetyl-8-cyclopentyl-5-methyl-2-[ |
供应商 | Tocris |
生物活性 | Potent Cdk4/6 inhibitor (IC50 values are 11 and 15 nM for Cdk4 and Cdk6 respectively). Selective for Cdk4/6 over a panel of 34 additional protein kinases (IC50 values are > 10 μM). Induces G1 cell cycle arrest and senescence in retinoblastoma protein (Rb)-proficient cell lines; blocks growth of intracranial glioblastoma multiforme xenografts in mice. Brain penetrant. |
运输条件 | Blue Ice |
存放说明 | Ambient |
纯度 | >98 % |
计算分子量 | 573.66 |
分子式 | C24H29N7O2 |
可溶性/溶解性 | Soluble to 100 mM in water and to 10 mM in DMSO |
参考文献 | Michaudet al (2010) Pharmacologic inhibition of cyclin-dependent kinases 4 and 6 arrests the growth of glioblastoma multiforme intracranial xenografts. Cancer Res. 70 3228. PMID: 20354191. Toogoodet al (2005) Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6. J.Med.Chem. 48 2388. PMID: 15801831. Fryet al (2004) Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol.Cancer Ther. 3 1427. PMID: 15542782. |