CDK4/6 inhibitor,potent and selective
CAS：1231930-82-7
分子式：C27H32F2N8.CH4O3S
分子量：602.7
纯度：98%
存储：Store at -20°C

Background:

LY2835219 is a selective and orally available dual cyclin-dependent kinases 4/6 (CDK4/6) inhibitor that potently inhibits the activities of CDK4 and CDK6 with the half maximal inhibition concentration IC50 values of 2 nM and 10 nM respectively [1].

LY2835219 has also been found to inhibit Rb phosphorylation both in vivo and in vitro leading to specific cell arrest at G1 phase as well as the inhibition of tumor growth [1].

Since the blood brain barrier (BBB) is a major obstacle for the effective treatment of primary brain tumors and brain metastases, LY2835219, which is able to cross the BBB, has the potential to inhibit intracranial tumor growth alone or in combination with other agents [1].

参考文献:
[1] Concepcion Sanchez-Martinez, Lawrence M. Gelbert, Harlan Shannon, Alfonso De Dios, Brian A. Staton, Rose T. Ajamie, Geri Sawada, Graham N. Wishart and Thomas J. Raub. LY2835219, a potent oral inhibitor of the cyclin-dependent kinases 4 and 6 (CDK4/6) that crosses the blood-brain barrier and demonstrates in vivo activity against intracranial human brain tumor xenografts [abstract]. In: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2011 Nov 12-16; San Francisco, CA. Philadelphia (PA): AACR; Mol Cancer Ther 2011;10(11 Suppl):Abstract nr B234.