BKM120 (NVP-BKM120, Buparlisib)

NVP-BKM120 is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

BKM120 is an aminopyridine that is 4-(trifluoromethyl)pyridin-2-amine substituted at position 5 by a 2,6-di(morpholin-4-yl)pyrimidin-4-y group. A selective PI3K inhibitor with anti-tumour properties. It has a role as an EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor and an antineoplastic agent. It is a member of morpholines, an aminopyrimidine, an aminopyridine and an organofluorine compound.|Buparlisib has been used in trials studying the treatment and basic science of Lymphoma, Metastases, Lung Cancer, Solid Tumors, and Breast Cancer, among others.|Buparlisib is an orally bioavailable specific oral inhibitor of the pan-class I phosphatidylinositol 3-kinase (PI3K) family of lipid kinases with potential antineoplastic activity. Buparlisib specifically inhibits class I PI3K in the PI3K/AKT kinase (or protein kinase B) signaling pathway in an ATP-competitive manner, thereby inhibiting the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate and activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents.

Buparlisib (944396-07-0) is potent pan-Class I PI3-kinase inhibitor (IC50’s: p110α = 52 nM, p110 = 166 nM, p110δ = 116 nM. P110g = 262 nM).1,2 It inhibited microtubule dynamics at in vitro concentrations >1μM and doses above 50mg/kg in mice.3 Buparlisib lead to a precipitous drop in DNA synthesis in a mouse model of BRCA1-linked triple-negative breast cancer with less affect in normal tissue.4

NVP-BKM 120 is a novel anti-tumor active compound that is selective in that it inhibits specifically PI3 kinase activating cell death in glioma cells. Glioma cells being those that proliferate from tumors in the brain or the spine.

A selective Class I PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50s of 50-300 nM.

Molecular Weight:410.4
XLogP3:1.5
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:11
Rotatable Bond Count:3
Exact Mass:410.16780842
Monoisotopic Mass:410.16780842
Topological Polar Surface Area:89.6
Heavy Atom Count:29
Complexity:530
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes