Buparlisib | PI3-kinase inhibitor

CAS:
944396-07-0
Catalog Number:
10-4325
Activity:
pan-Class I PI3-kinase inhibitor
Chemical Names:
5-(2,6-Dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridine-2-amine; NVP-BKM120
Molecular Weight:
410.39
Molecular Formula:
C18H21F3N6O2
Solubility:
Soluble in DMSO (15 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$60.00
25 mg$230.00

Buparlisib (944396-07-0) is potent pan-Class I PI3-kinase inhibitor (IC50’s: p110α = 52 nM, p110ß = 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

References:

  1. Burger 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
  2. Maira et al. (2012), Identification and Characterization of NVP-BKM120, an Orally Available Pan-Class I PI3-Kinase Inhibitor; Mol. Cancer Ther. 11 317
  3. 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
  4. Juvekar et al. (2016), Phosphoinositide 3-kinase inhibitors induce DNA damage through nucleoside depletion; Proc. Natl. Acad. Sci USA. 113 E4338
CAS:
944396-07-0
Catalog Number:
10-4325
Activity:
pan-Class I PI3-kinase inhibitor
Chemical Names:
5-(2,6-Dimorpholin-4-ylpyrimidin-4-yl)-4-(trifluoromethyl)pyridine-2-amine; NVP-BKM120
Molecular Weight:
410.39
Molecular Formula:
C18H21F3N6O2
Solubility:
Soluble in DMSO (15 mg/ml)
Physical Properties:
White solid
Purity:
99% HPLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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