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Enzymes for Research, Diagnostic and Industrial Use

AT7867

Cat No.
CEI-0110
Description
As an ATP-competitive inhibitor, AT7867 can potently Akt1, Akt2, Akt3 and S6K with IC50 of 32 nM, 17 nM, 47 nM and 85 nM.
CAS No.
857531-00-1
Molecular Weight
337.85
Purity
>99%
Storage
2 years at -20 centigrade
Targets
Akt1, Akt2, Akt3, S6K
Molecular Formula
C20H20ClN3
Chemical Name
4-(4-(1H-pyrazol-4-yl)phenyl)-4-(4-chlorophenyl)piperidine
Solubility
DSMO 68 mg/mL Water
In vitro
As an ATP-competitive small molecule inhibitor, AT7867 can potently inhibitor of Akt, p70S6 kinase and PKA. AT7867 can also blocked proliferation in a number of human cancer cell lines which exhibit deregulation of the PI3K/AKT pathway by mechanisms, such as PTEN or PIK3CA mutations. In addition, the MES-SA uterine cell line seemed to be the most sensitive to growth inhibition by AT7867.
In vivo
In MES-SA tumor xenografts, doses of AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) were given to athymic mice bearing MES-SA tumors. Clear inhibition of phosphorylation of GSK3betaand S6RP in tumors was seen at 2 and 6 hours following treatment with AT7867 and AT7867 can induce an increase in cleaved PARP, leading to inducing apoptosis in the xenograft tumor cells.
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