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LDK378 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LDK378 dihydrochloride图片
CAS NO:1380575-43-8
包装与价格:
包装价格(元)
10mg电议
50mg电议
200mg电议

产品介绍
LDK378 dihydrochloride (LDK378 dihydrochloride) 是一种选择性、口服生物利用度和 ATP 竞争性的 ALK 酪氨酸激酶抑制剂,IC50 为 200 pM。
Cas No.1380575-43-8
别名双盐酸盐色瑞替尼; LDK378 dihydrochloride
化学名5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine;dihydrochloride
Canonical SMILESCC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl.Cl.Cl
分子式C28H38Cl3N5O3S
分子量631.06
溶解度Soluble in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

LDK378 is a highly potent inhibitor of anaplastic lymphoma kinase (ALK), which is a receptor tyrosine kinase belonging to the superfamily of insulin receptor, with half maximal inhibitory concentration IC50 of 200 pM. LDK378 also exhibits modest to high inhibition against a panel of other kinases, in which only three kinases with IC50 below 100 nM includes IGF-1R (8 nM), InsR (7 nM) and STK22D (23 nM). In previous studies, LDK378 has been found to inhibit the proliferation of Ba/F3 cells transfected with the NPM-ALK fusion gene and Karpas 299 human non-Hodgkin’s Ki-positivr large cell lymphoma harboring the NPM-ALK fusion gene with IC50 of 22.8 nM and 26 nM.

References:
[1]Chen J, Jiang C, Wang S. LDK378: a promising anaplastic lymphoma kinase (ALK) inhibitor. J Med Chem. 2013 Jul 25;56(14):5673-4. doi: 10.1021/jm401005u. Epub 2013 Jul 9.
[2]Marsilje TH, Pei W, Chen B, Lu W, Uno T, Jin Y, Jiang T, Kim S, Li N, Warmuth M, Sarkisova Y, Sun F, Steffy A, Pferdekamper AC, Li AG, Joseph SB, Kim Y, Liu B, Tuntland T, Cui X, Gray NS, Steensma R, Wan Y, Jiang J, Chopiuk G, Li J, Gordon WP, Richmond W, Johnson K, Chang J, Groessl T, He YQ, Phimister A, Aycinena A, Lee CC, Bursulaya B, Karanewsky DS, Seidel HM, Harris JL, Michellys PY. 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 Jul 25;56(14):5675-90. doi: 10.1021/jm400402q. Epub 2013 Jun 26.