Buparlisib | PI3-kinase inhibitor

Buparlisib (944396-07-0) is potent pan-Class I PI3-kinase inhibitor (IC50’s: p110a = 52 nM, p110b = 166 nM, p110d = 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
Weight 0.01 mg
Dimensions 0.01 × 0.01 × 0.01 cm
Size:

5 mg, 25 mg

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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

Buparlisib | PI3-kinase inhibitor

$70.00$265.00

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
  • 5 mg
  • 25 mg
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