AT7867 Inhibitor CAS No. 857531-00-1

Cat. No.	Name	Size	Price
KI1198	AT7867	10 mg	$512
	AT7867	50 mg	$1552
	AT7867	200 mg	$3952

Chemical Characteristic

Product Name	AT7867
CAS No.	857531-00-1
Molecular Weight	337.85
Formula	C₂₀H₂₀ClN₃
Chemical Name	4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine
Smiles	N1CCC(CC1)(c1ccc(cc1)c1cn[nH]c1)c1ccc(cc1)Cl
Chemical Structure

Biological activities

AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase. The IC50 of AT7867 is 32, 17 and 47 nM against AKT1, AKT2 and AKT3, respectively. In addition, AT7867 also inhibits PKA and p70S6K with IC50 of 20 and 85 nM, respectively. AT7867 ATP-competitively inhibits AKT2 with a Ki of 18 nM. AT7867 blocks proliferation in a number of human cancer cell lines including MES-SA uterine, MDA-MB-468 and MCF-7 breast, and HCT116 and HT29 colon lines with an IC50 ranging from 0.9 to 3 µM. AT7867 inhibits the proliferation of MES-SA cell line with an IC50 of 0.94 µM. AT7867 inhibits AKT signaling in U87MG human glioblastoma cells in a concentration-dependent and time-dependent manner and induces apoptosis. AT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) inhibits of phosphorylation of downstream substrates of both AKT and p70S6K and induces apoptosis in athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model.^[1]

Protocols

In vitro AT7867 is dissolved to a 10 mM stock solution in DMSO.^[1]

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.

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