Aurora A Kinase inhibitor, Potent and selective
CAS：1028486-01-2
分子式：C27H20ClFN4O4
分子量：518.92
纯度：98%
存储：Store at -20°C

Background:

The orally bioavailable agent, MLN8237 (also known as alisertib), is a potent small-molecule inhibitor of Aurora A kinase (AAK) which is overexpressed in several types of tumor and? associated with oncogenesis and tumor progression. It was developed from its predecessor, MLN8054, in order to minimize the benzodiazepine-like effects seen with MLN8054. The inhibitory effect of MLN8237 is ATP-competitive, reversible and AAK-specific with an inhibition constant (K_i) of 0.43 nmol/L. MLN8237 is being investigated to treat advanced malignancies, due to its bothin vitroandin vivoactivities against a broad range of tumor types.

Reference

[1]E. Claire Dees, Roger B. Cohen, Margaret von Mehren, Thomas E. Stinchcombe, Hua Liu, Karthik Venkatakrishnan, Mark Manfredi, Howard Fingert, Howard A. Burris III, and Jeffrey R. Infante. Phase I study of aurora A kniase inhibitor MLN8237 in advanced solid tumors: safety, pharmacokinetics, pharmacodynamics, and bioavailability of two oral formulations. Clin Cancer Res 2012; 18:4775-4784.