| 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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Products are for research use only. Not for human use.
