Brief Description |
NVP-BKM120 (Buparlisib) is an orally bioavailable and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor with in vitro IC50 values of 52 nM/166 nM/116 nM/262 nM for p110α /β /δ /γ isoforms, respectively. It is much less effective on inhibiting the class III PI3K Vps34 and mTOR, and has no effect on PI4Kβ . It is currently in clinical trials for cancer treatment. |
References |
1.M. T. Burger, et al., Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer
ACS Med. Chem. Lett., 2011, 2 (10), pp 774-779
2. S. M. Maira, et al., Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor, Mol Cancer Ther. 2012 Feb; 11(2):317-28
3. S. M. Brachmann, et al., Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations, Mol Cancer Ther. 2012 Aug; 11(8):1747-57 |