LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively.
application：
5-Chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine, is a Anaplastic lymphoma kinase (ALK) inhibitor.
1.Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M et al.. (2013) 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, 56 (14):(5675-90). [PMID:23742252]
2.Shaw AT, Kim DW, Mehra R, Tan DS, Felip E, Chow LQ, Camidge DR, Vansteenkiste J, Sharma S, De Pas T et al.. (2014) Ceritinib in ALK-rearranged non-small-cell lung cancer.. N Engl J Med, 370 (13):(1189-97). [PMID:24670165]
3.Thomas RK. (2014) Overcoming drug resistance in ALK-rearranged lung cancer.. N Engl J Med, 370 (13):(1250-1). [PMID:24670172]
4.Friboulet L, Li N, Katayama R, Lee CC, Gainor JF, Crystal AS, Michellys PY, Awad MM, Yanagitani N, Kim S et al.. (2014) The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.. Cancer Discov, 4 (6):(662-673). [PMID:24675041]
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