GSK2636771 | Potent and selective inhibitor of PI3Kß

CAS:
 1372540-25-4
Catalog Number:
 10-4172
GSK2636771 Focus Biomolecules

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25 mg$295.00
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GSK2636771 (1372540-25-4) is a potent, selective (>1000-fold over α, 10-fold over δ, and >2000-fold over γ), and orally bioavailable inhibitor of PI3Kß (IC50 = 5.2 nM).1  Active in vitro against multiple types of PTEN-deficient cancer cells. GSK2636771 potently blocked migration and invasion of DU145 prostate cancer cells.2 GSK2636771 has also been identified as a GPR39 agonist.3

References/Citations:

  1. Mateo et al. (2017), A First-in-Human Study of GSK2636771, a Phosphoinositide 3 Kinase Beta-Selective Inhibitor, in Patients with Advanced Solid Tumors; Clin. Cancer Res. 23 5981
  2. Zhang et al. (2018), Phosphatidylinositol 3-kinase ß and δ isoforms play key roles in metastasis of prostate cancer DU145 cells; FASEB J. 32 5967
  3. Sato et al. (2016); Discovery and Characterization of Novel GPR39 Agonists Allosterically Modulated by Zinc, Mol. Pharmacol., 90 726
CAS:
1372540-25-4
Catalog Number:
10-4172
Activity:
PI3Kß kinase inhibitor
Chemical Names:
2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid
Molecular Weight:
433.43
Molecular Formula:

C22H22F3N3O3

Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
Pale yellow solid
Purity:

>98% by HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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