ALK inhibitor 1

Short Summary : ALK inhibitor, novel and selective

Category : Tyrosine Kinase|ALK

Purity : 0.98

CAS Number : 761436-81-1

Formula : C23H28BrN7O3S

Molecular Weight : 562.48

SMILE : CNS(=O)(=O)C1=CC=CC=C1NC2=NC(=NC=C2Br)NC3=C(C=C(C=C3)N4CCN(CC4)C)OC

Solubility : Soluble in DMSO

Storage : Store at -20°C

Description : ALK inhibitors are potential anti-cancer drugs that act on tumours with variations of anaplastic lymphoma kinase (ALK) such as an EML4-ALK translocation [1]. ALK inhibitor 1 is a novel and selective inhibitor for the ALK kinase.In vitro: ALK inhibitor 1 (2-[[5-bromo-2-[2-methoxy-4-(4-methylpiperazin-1-yl) anilino]pyrimidin-4-yl] amino]-N-methylbenzenesulfonamide) is a chemical analogue of LDK378 that is a potent ALK inhibitor [2]. In vivo: No animal in-vivo data available currently. Clinical trial: ALK inhibitor 1 is currently in the preclinical developlent stage and no clinical data are available.Reference:[1] Palmer RH, Vernersson E, Grabbe C, Hallberg B. Anaplastic lymphoma kinase: signalling in development and disease. Biochem J. 2009;420(3):345-61. [2] Marsilje TH, Pei W, Chen B, Lu W, et al. Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials. J Med Chem. 2013;56(14):5675-90.

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