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Background Information:
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.
Reference:
1. M. H. Norman, et al, Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511, J Med Chem. 2012 Sep 13; 55(17):7796-816.
2. Many other vendors, if not all, offer the product AMG-511 without reporting optical purity - trying to hide something? - too poor to report? No clue?
APIM050076: AMG-511
CAS No.: 1253573-53-3.
Molecular Formula: C22H28FN9O3S ? 0.3HCl.
Molecular Weight: 528.5.
Purity: >99% Chem and Optical Purity (HPLC and Chiral HPLC).
QC: HPLC-MS, 1HNMR, Chiral HPLC, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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