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GSK-690693

CAT: 0013-GTR19160726-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19160726-01Size:200 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
A potent, ATP competitive, pan-AKT inhibitor with IC50 of 2, 13, and 9 nM against AKT1, 2, and 3, respectively; also inhibits additional members of the AGC kinase family (PKA, PrkX, and PKC isozymes, IC50s 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. (In Vivo) :A single administration of GSK690693 inhibits GSK3β phosphorylation in human breast carcinoma (BT474) xenografts in a dose- and time-dependent manner. Similarly, GSK690693 induces a reduction in phosphorylation of the Akt substrates, PRAS40, and FKHR/FKHRL1. GSK690693 also results in an acute increase in blood glucose, returning to baseline 8 to 10 hours after drug administration. Administration of GSK690693 induces reductions in phosphorylated Akt substrates in vivo, and potently inhibits the growth of human SKOV-3 ovarian, LNCaP prostate, and BT474 and HCC-1954 breast carcinoma xenografts, with maximal inhibition of 58% to 75% at the dose of 30 mg/kg/day. GSK690693 exhibits efficacy irrespective of the mechanism of Akt activation involved. GSK690693 is most effective in delaying tumor progression in Lck-MyrAkt2 mice expressing a membrane-bound, constitutively active form of Akt.
CAS Number
937174-76-0
Product Name Alternative
GSK 690693 | GSK690693
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
CC (O) (C) C#CC1=NC=C (OC[C@@H]2CNCCC2) C3=C1N=C (C4=NON=C4N) N3CC
Molecular Formula
C21H27N7O3
Molecular Weight
425.4842
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
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-

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