bkm120-nvp-bkm120-buparlisib

Description: BKM120 (also known as NVP-BKM120, or Buparlisib) is a selective, orally bioavailable and potent Pan-class I PI3K inhibitor of p110alpha/beta/delta/gamma with IC50 of 52 nM/166 nM/116 nM/262 nM in cell-free assays, respectively. It has anticancer activity. It has reduced potency against VPS34, mTOR, DNAPK and is with little activity to PI4Kbeta. BKM120 has been undergoing various clinical trials for the treatment of a variety of cancers. The intracellular phosphatidylinositol-3-kinase(PI3K) pathway regulates cellular functions including cell proliferation, growth, survival, apoptosis, protein synthesis, and glucose metabolism. BKM120, a biologic characterization of the 2-morpholino pyrimidine derivative, is a pan-PI3K inhibitor. In vitro experiments showed that NVP-BKM120 inhibits all four class I PI3K isoforms in biochemical assays with at least 50-fold selectivity against other protein kinases.

References: Mol Cancer Ther. 2012 Feb; 11(2):317-28; J Clin Oncol. 2012 Jan 20; 30(3):282-90.

Related CAS: 1312445-63-8 (HCl) 944396-07-0 (free base)