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Background Information:
CEP-28122 is a highly potent, selective and orally active ALK inhibitor (Ezymatic IC50: 1.9 nM (ref 1), 3 nM (ref 2), Cellular IC50: 30 nM (ref 2), Cellular IC50 in 75% murine: 300 nM (ref 2)), displaying a favorable pharmaceutical and pharmacokinetic profile and robust and selective pharmacologic efficacy against ALK-positive human cancer cells and tumor xenograft models in mice.
Reference:
1. M. Cheng, et al., CEP-28122, a Highly Potent and Selective Orally Active Inhibitor of Anaplastic Lymphoma Kinase with Antitumor Activity in Experimental Models of Human Cancers. Mol Cancer Ther. 2012 Mar;11(3):670-9.
2. M. J. Jacobs, et al, Fused bicyclic 2,4-diaminopyrimidine derivative as a dual alk and fak inhibitor, WO2013134353 A1.
APIM050126: CEP-28122
CAS No.: 1022958-60-6.
Molecular Formula: C28H35ClN6O3.
Molecular Weight: 539.1.
Purity: 100% optical purity (Chiral HPLC), 99.5% chemical purity (HPLC at 214 and 254 nm).
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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