NVP-BKM120,PI3KInhibitorBKM120

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产品名称: NVP-BKM120,PI3KInhibitorBKM120

产品型号: M66051-2s

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NVP-BKM120,PI3KInhibitorBKM120

NVP-BKM120,PI3KInhibitorBKM120 的详细介绍

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: 4^oC 1 year. DMSO: 4^oC 3 month; -20^oC 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.

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

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