NVP-BKM120, PI3K Inhibitor BKM120


Catalog No. size PriceQuantity
M66051-2D 10 mM in DMSO (0.488 mL) $89
M66051-2S 2mg solid $89
M66051-10S 10mg solid $360

Description

Product Information
Molecular Weight: 410.39
Formula: C18H21F3N6O2
Purity: ≥98%
CAS#: 944396-07-0
Solubility: DMSO up to 100 mM
Chemical Name: 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:
BKM120 (NVP-BKM120) is a potent and selective, orally available pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. It inhibits all four class-I PI3K isoforms in biochemical assays with IC50 ~50-250 nM, but exhibits selectivity of >100 folds against other protein kinases. It is also active against the most common somatic PI3Ka mutations but does not significantly inhibit the related class-III (Vps34) and class-IV (mTOR, DNA-PK) PI3K kinases. BKM120 has shown to significantly inhibit cell growth and induce apoptosis in a variety of tumor cell lines as well as in animal models. Consistent with its mechanism of action, NVP-BKM120 decreases the cellular levels of p-Akt in relevant models, as well as modulates downstream effectors in a concentration dependent and pathway-specific manner.

 

How to Use:

 

  • In vitro:  BKM120 was typically used at 1 µM in vitro and cellular assays.
  • In vivo: BKM120 was formulated in NMP/PEG300 (10/90, v/v) and orally dosed to mice at 10 mg/kg once per day.

 

 

Reference:

  1. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. (2012) Mol Cancer Ther. 11(2):317-28.
  2. Koul D, et al. Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cells. (2012) Clin Cancer Res. 18(1):184-95.
  3. Park E, et al. NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations. (2012) Int J Oncol. 40(4):1259-66
  4. Brachmann SM, et al. Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations.  (2012) Mol Cancer Ther.
  5. Ren H, et al. The combination of RAD001 and NVP-BKM120 synergistically inhibits the growth of lung cancer in vitro and in vivo. 



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