[CAS NO. 1047634-65-0]  Uprosertib (GSK2141795)

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PRODUCTS SPECIFICATIONS [1047634-65-0]

Store
Catalog
SLK-S7492
Brand
Selleck
CAS
1047634-65-0

DESCRIPTION [1047634-65-0]

Overview

MDLMFCD28144686
Molecular Weight429.25
Molecular FormulaC18H16Cl2F2N4O2
SMILESO=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)O1)N[C@@H](CC3=CC=C(F)C(F)=C3)CN

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Uprosertib (GSK2141795, GSK795) is a selective, ATP-competitive, and orally bioavailable inhibitor with of 180 nM, 328 nM, and 38 nM for Akt 1, 2 and 3, respectively. Phase 2.

Targets

Akt3 [1]
(Cell-free assay)
Akt1 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
38 nM180 nM328 nM

In vitro

Uprosertib inhibits multiple AKT substrate phosphorylation levels, including GSK3β, PRAS40, FOXO and Caspase 9 in both BT474 and LNCaP cells. Uprosertib preferentially inhibits the proliferation of human cancer cells lines with AKT pathway activation. In LNCaP, BT474, A3 and I9.2 cells lines, Uprosertib also causes cell cycle arrest. In both SKOV3 and PEO4 cells, Uprosertib causes growth-arrest as single agent, and enhances cisplatin-induced apoptosis.

In vivo

In mice bearing BT474 breast tumor xenografts, Uprosertib (100 mg/kg, p.o.) results 61% tumor growth inhibition. In mice bearing SKOV3 ovarian tumor xenografts, Uprosertib (30 mg/kg, p.o.) results 61% tumor growth inhibition.