AT7867 dihydrochloride_1431697-86-7_DataSheet_MedChemExpress

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Product Name:AT7867 dihydrochloride

CAS No.: 1431697-86-7

Cat. No.:HY-12059AProduct Data Sheet

MWt:410.77

Formula:C20H22Cl3N3

Purity :>98%

Solubility:

DMSOy

Mechanisms:

Biological Activity:

AT7867HclisapotentATPcompetitiveinhibitorofAkt1/2/3andp70S6K/PKAwithIC50of32

Pathways:PI3K/Akt/mTOR; Target:Akt

AT7867 Hcl is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively; little activity outside the AGC kinase family.

IC50 value: 32 nM/17 nM/47 nM(Akt1/2/3) [1]

Target: Akt

in vitro: AT7867 also inhibits structurally related AGC kinases p70S6K and PKA with IC50 of 20 nM

and 85 nM, respectively. AT7867 shows ATP-competitive activity to Akt2 with Ki of 18 nM. AT7867

exhibits antiproliferation in cell lines with PTEN or PIK3CA mutations and shows great potent to

MES-SA, MDA-MB-468, MCF-7, HCT116 and HT29 with IC50 of 0.94 μM, 2.26 μM, 1.86 μM, 1.76 μ

M and 3.04 M, respectively. AT7867 also suppresses the cell growth of U87MG, PC-3 and DU145

References:

[1]. Grimshaw KM, et al. AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that

induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther, 2010, 9(5), 1100-1110.μ,pyppg,

cells with IC50 of 8.22 μM, 10.37 μM and 11.86 μM, respectively. AT7867 suppresses Akt activity by

inhibiting phosphorylation of GSK-3β in human tumor cells with IC50...

Caution: Not fully tested. For research purposes only

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