BKM120 (NVP-BKM120, Buparlisib)

BKM120 (NVP-BKM120, Buparlisib)
  • CAS No.:944396-07-0
Other grades of this product :
BKM120 (NVP-BKM120, Buparlisib) Basic information
Product Name:BKM120 (NVP-BKM120, Buparlisib)
Synonyms:5-[2,6-Di(4-morpholinyl)-4-pyrimidinyl]-4-(trifluoromethyl)-2-pyridinamine;5-(2,6-diMorpholinopyriMidin-4-yl)-4-(trifluoroMethyl)pyridin-2-aMine;BKM120 (NVP-BKM120);NVP-BKM-120;BKM120 (NVP-BKM120, Buparlisib);NVP-BKM120, Buparlisib;BKM120BASE;Buparlisib
CAS:944396-07-0
MF:C18H21F3N6O2
MW:410.39
EINECS:
Product Categories:Akt;mTOR;API;Inhibitor;Inhibitors;PI3K
Mol File:944396-07-0.mol
BKM120 (NVP-BKM120, Buparlisib) Chemical Properties
Melting point 143-147°C
Boiling point 645.7±65.0 °C(Predicted)
density 1.382
storage temp. -20°C
solubility Soluble in DMSO (15 mg/ml)
form White powder.
pka5.94±0.50(Predicted)
color White
Stability:Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Safety Information
HS Code 29349990
MSDS Information
BKM120 (NVP-BKM120, Buparlisib) Usage And Synthesis
DescriptionBuparlisib (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
UsesA selective Class I PI3K inhibitor of p110α, p110β, p110δ and p110γ with IC50s of 50-300 nM.
UsesNVP-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 tu mors in the brain or the spine.
UsesNVP-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.
ReferencesBurger et al. (2011), Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer; ACS Med. Chem. Lett. 2 774 Maira et al. (2012), Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor; Mol. Cancer Ther. 11 317 Brachmann et al. (2012), Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations; Mol. Cancer Ther. 11 1747 Juvekar et al. (2016), Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion; Proc. Natl. Acad. Sci USA. 113 E4338
BKM120 (NVP-BKM120, Buparlisib) Preparation Products And Raw materials

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