CEP-28122 mesylate hydrochloride 

CEP-28122 mesylate hydrochloride, a diaminopyrimidine derivative, is a potent, selective, and orally active ALK inhibitor with an IC₅₀ value of 1.9 nM. CEP-28122 mesylate hydrochloride has antitumor activity in experimental models of ALK-positive human cancers. CEP-28122 mesylate hydrochloride has good pharmacodynamic and pharmacokinetic activity. CEP-28122 mesylate hydrochloride can be used for the study of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small cell lung cancer (NSCLC), and neuroblastoma cells^[1].

CEP-28122 (3-3000 nM; 48 hours) mesylate hydrochloride treatment leads to concentration-dependent growth inhibition of Karpas-299 and Sup-M2 cells in culture, associates with concentration-related caspase 3/7 activation^[1].
CEP-28122 (30-1000 nM; 2 hours) mesylate hydrochloride treatment leads to substantial suppression of phosphorylation of putative downstream effectors of ALK in Sup-M2 cells, indicating that the downstream signaling pathways are mediated by individual ALK fusion protein^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CEP-28122 (3-30 mg/kg; oral gavage; twice a day; 12 days) mesylate hydrochloride produces dose-dependent antitumor activity in Sup-M2 subcutaneous tumor xenografts in SCID mice.In contrast, CEP-28122 has no antitumor activity in nu/nu mice bearing HCT116, suggesting that the antitumor activity of CEP-28122 in NPM-ALK–positive Sup-M2 tumor models is due to sustained NPM-ALK inhibition in tumors ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

671.64

C₂₉H₄₀Cl₂N₆O₆S

1354545-57-5

O=C([C@H]1[C@](C2)([H])C=C[C@]2([H])[C@H]1NC3=NC(NC4=CC=C5C(CC[C@@H](N6CCOCC6)CC5)=C4OC)=NC=C3Cl)N.O=S(C)(O)=O.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Mangeng 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.  [Content Brief]