Language:English
Language:

Xcessbio

Place your promotion here

You have no items in your shopping cart.

NVP-BKM120, PI3K Inhibitor BKM120

NVP-BKM120, PI3K Inhibitor BKM120

$89.00
A selective PI3K Inhibitor in clinical trials for advanced solid tumors.
Catalog No. Unit Price Qty
M66051-2s 2mg solid $89.00
M66051-2 10 mM in DMSO (0.488 mL) $89.00
M66051-50s 50mg solid $1050.00

Details

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. 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. 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. 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. 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. 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.

Description

Details

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. 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. 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. 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. 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. 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.

Reviews

Write Your Review

How do you rate this product? *

Price:
Value:
Quality: