[CAS NO. 1047644-62-1] Afuresertib (GSK2110183)

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PRODUCTS SPECIFICATIONS [1047644-62-1]

Catalog

SLK-S7521

Brand

Selleck

CAS

1047644-62-1

DESCRIPTION [1047644-62-1]

Overview

MDL	MFCD26961098
Molecular Weight	427.32
Molecular Formula	C18H17Cl2FN4OS
SMILES	O=C(C1=CC(C2=C(Cl)C=NN2C)=C(Cl)S1)N[C@@H](CC3=CC=CC(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.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3402 mL	11.7008 mL	23.4017 mL
5 mM	0.4680 mL	2.3402 mL	4.6803 mL
10 mM	0.2340 mL	1.1701 mL	2.3402 mL
50 mM	0.0468 mL	0.2340 mL	0.4680 mL

Description

Afuresertib (GSK2110183) is a potent, orally bioavailable inhibitor with of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2.

Targets

Akt1 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)
0.08 nM(Ki)	2 nM(Ki)	2.6 nM(Ki)

In vitro

Afuresertib inhibits the kinase activity of the E17K AKT1 mutant protein with EC50 of 0.2 nM. Afuresertib shows a concentration-dependent effect on multiple AKT substrate phosphorylation levels, including GSK3b, PRAS40, FOXO and Caspase 9. Overall 65% of the hematological cell lines are sensitive to afuresertib (EC50 < 1 μM). Among tested solid tumor cell lines, 21% have EC50 < 1 μM in response to afuresertib.

In vivo

Mice bearing BT474 breast tumor xenografts are dosed with afuresertib (p.o.) at 10, 30 or 100 mg/kg daily which results in 8, 37 and 61% TGI, respectively. Mice bearing SKOV3 ovarian tumor xenografts are treated with 10, 30 and 100 mg/kg afuresertib which results in 23, 37 and 97% TGI, respectively.

References

[1] Dumble M, et al. PLoS One, 2014, 9(6):e100880.