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GSK2636771

Chemical Structure : GSK2636771

CAS No.: 1372540-25-4

GSK2636771 (GSK 2636771)

Catalog No.: PC-21944Not For Human Use, Lab Use Only.

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with Ki/IC50 of 0.89/5.2 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with Ki/IC50 of 0.89/5.2 nM, respectively.
GSK2636771 displays 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
GSK2636771 causes cell viability significantly more decreased in the control cells (p110β-reliant PTEN-deficient PC3 prostate and BT549 and HCC70 breast cancer cell lines) than in PTEN-mutant and PTEN wild-type EEC cells.
GSK2636771 decreases AKT phosphorylation in prostate and breast cancer cell lines, suppresses cell and tumor growth in vivo.

Physicochemical Properties

M.Wt 433.43
Formula C22H22F3N3O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-Methyl-1-(2-methyl-3-(trifluoromethyl)benzyl)-6-morpholino-1H-benzo[d]imidazole-4-carboxylic acid

References

1. Weigelt B, et al. Clin Cancer Res. 2013 Jul 1;19(13):3533-44.

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