[CAS NO. 937174-76-0]  GSK690693

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PRODUCTS SPECIFICATIONS [937174-76-0]

Catelog
SLK-S1113
Brand
Selleck
CAS
937174-76-0

DESCRIPTION [937174-76-0]

Overview

MDLMFCD14105605
Molecular Weight425.48
Molecular FormulaC21H27N7O3
SMILESC(C)N1C=2C(=C(C#CC(C)(C)O)N=CC2OC[C@H]3CCCNC3)N=C1C=4C(N)=NON4

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

1 mg5 mg10 mg
1 mM2.3503 mL11.7514 mL23.5029 mL
5 mM0.4701 mL2.3503 mL4.7006 mL
10 mM0.2350 mL1.1751 mL2.3503 mL
50 mM0.0470 mL0.2350 mL0.4701 mL

Description

GSK690693 is a pan-Akt inhibitor targeting with of 2 nM/13 nM/9 nM in cell-free assays, also sensitive to the AGC kinase family: PKA, PrkX and PKC isozymes. GSK690693 also potently inhibits and from the CAMK family with IC50 of 50 nM and 81 nM, respectively. GSK690693 affects activity, robustly inhibits activation. Phase 1.

Targets


In vitro

GSK690693 is very selective for the Akt isoforms versus the majority of kinases in other families. However, GSK690693 is less selective for members of the AGC kinase family including PKA, PrkX, and PKC isozymes with IC50 of 24 nM, 5 nM, and 2-21 nM, respectively. GSK690693 also potently inhibits AMPK and DAPK3 from the CAMK family with IC50 of 50 nM and 81 nM, respectively, and PAK4, 5, and 6 from the STE family with IC50 of 10 nM, 52 nM, and 6 nM, respectively. GSK690693 inhibits the phosphorylation of GSK3β in tumor cells with IC50 ranging from 43 nM to 150 nM. GSK690693 treatment leads to a dose-dependent increase in the nuclear accumulation of the transcription factor FOXO3A. GSK690693 potently inhibits the proliferation of T47D, ZR-75-1, BT474, HCC1954, MDA-MB-453, and LNCaP cells with IC50 of 72 nM, 79 nM, 86 nM, 119 nM, 975 nM, and 147 nM, respectively. GSK690693 treatment induces apoptosis at concentrations >100 nM in both LNCaP and BT474 cells. Consistent with the role of AKT in cell survival, GSK690693 induces apoptosis in sensitive ALL cell lines.


Synonyms

3-Butyn-2-ol, 4-[2-(4-amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-
4-[2-(4-Amino-1,2,5-oxadiazol-3-yl)-1-ethyl-7-[(3S)-3-piperidinylmethoxy]-1H-imidazo[4,5-c]pyridin-4-yl]-2-methyl-3-butyn-2-ol
GSK 690693