NVP-BKM120 (BUPARLISIB)

Background Information:

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.

Reference:

1. M. T. Burger, et al., Identification of NVP-BKM120 as a Potent,
Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating
CancerACS 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.

APIM050210: NVP-BKM120 (BUPARLISIB)

CAS No.: 944396-07-0.
Molecular Formula: C₁₈H₂₁F₃N₆O_2.
Molecular Weight: 410.4 (refer to Certificate, batch-specific).
Purity: >99.5% (HPLC at 214 and 254 nm).
QC: HPLC-MS, ¹HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.