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AMG-511
AMG-511 (AMG 511) is an orally bioavailable, highly potent and selective pan-class I phosphatidylinositol-3 kinase (PI3K) inhibitor with in vitro Ki values of 4nM/6nM/2nM/1nM for p110α/β/δ/γ isoforms, respectively, and is highly selective over mTOR (IC50 > 10000 nM), hVPS34 (IC50 > 9000 nM), DNAPK (IC50 = 12000 nM), and a broad panel of other protein kinases. It effectively inhibited pAKT in tumor tissue in a dose- and time-dependent manner (up to 16 hours). In animal studies it efficaciously inhibited tumor growth in PTEN-null, KRAS mutant, and HER2 amplified xenograft models. It is currently in clinical trials for cancer treatment.
Catalog NO: CT-AMG511
Synonym:
CAS NO: 1253573-53-3
Mol. Formula: C22H28FN9O3S ∙ 0.3HCl
MW: 528.5
** AMG-511 being offered is a single isomer (>99% optically pure by Chiral HPLC, R-enantiomer, clinically active isomer) (Ref. 2), 99.5% chemically pure by achiral HPLC, + impeccable 1H-NMR + an excellent quantitative elemental analysis. Ship within 1 day.