GSK2636771

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Cat No.

CEI-0872

Description

GSK2636771 is a potent, orally bioavailable, PI3Kβ-selective inhibitor, sensitive to PTEN null cell lines. Phase 1/2a.

CAS_No

1372540-25-4

Molecular Weight

433.42

Storage

2 years -20 centigrade Powder; 2 weeks 4 centigrade in DMSO; 6 months -80 centigrade in DMSO.

Targets

PI3Kβ

Molecular Formula

C22H22F3N3O3

Chemical Name

1H-Benzimidazole-4-carboxylic acid, 2-methyl-1-[[2-methyl-3-(trifluoromethyl)phenyl]methyl]-6-(4-morpholinyl)-

Solubility

DMSO 87 mg/mL; Water <1 mg/mL; Ethanol 19 mg/mL

In vitro

GSK-2636771 shows selectively inhibitory activity in PTEN null cell lines (human prostate adenocarcinoma PC-3 and breast cancer HCC70) with EC50 of 36 nM and 72 nM, respectively.

In vivo

GSK-2636771 decreases phosphorylated protein kinase Akt (Ser473) levels in these xenograft models. GSK-2636771 (100 mg/kg) do not increase glucose/insulin levels in mice.

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Project Description:

Our Products Cannot Be Used As Medicines Directly For Personal Use.

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