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AMG511

Chemical Structure : AMG511

CAS No.: 253573-53-3

AMG511 (AMG-511, AMG 511)

Catalog No.: PC-60983Not For Human Use, Lab Use Only.

AMG511 (AMG-511) potent, efficacious, and orally available pan class I PI3K inhibitor with Ki of 4/6/2/1 nM for PI3Kα/β/δ/γ, respectively.

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Biological Activity

AMG511 (AMG-511) potent, efficacious, and orally available pan class I PI3K inhibitor with Ki of 4/6/2/1 nM for PI3Kα/β/δ/γ, respectively.
AMG511 displays high selectivity over other members of the closely related PIKK family of kinases, including mTOR, hVPS34 and PI4Ks, as well as a panel of 370 protein kinases (IC50>1 uM).
AMG511 inhibits AKT (Ser473) phosphorylation in U87 MG glioblastoma cells with IC50 of 4 nM.
AMG511 potently blocks the targeted PI3K pathway in mouse liver pharmacodynamic model and inhibits tumor growth in U87 malignant glioma glioblastoma xenograft model.

Physicochemical Properties

M.Wt 517.584
Formula C22H28FN9O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-4-(2-((5-Fluoro-6-methoxypyridin-3-yl)amino)-5-(1-(4- (methylsulfonyl)piperazin-1-yl)ethyl)pyridin-3-yl)-6-methyl-1,3,5-triazin-2-amine

References

1. Norman MH, et al. J Med Chem. 2012 Sep 13;55(17):7796-816.

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