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ALK inhibitor 2

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Chemical Structure| 761438-38-4 同义名 : -
CAS号 : 761438-38-4
货号 : A524942
分子式 : C23H28ClN7O3S
纯度 : 99%+
分子量 : 518.032
MDL号 : MFCD23380589
存储条件:

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(96.52 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 Anaplastic lymphoma kinase (ALK) encodes a highly conserved receptor tyrosine kinase (RTK) within the insulin receptor superfamily, comprised of an extracellular domain, a single-pass transmembrane region, and an intracellular kinase domain[2]. ALK inhibitors are potential anti-cancer drugs that act on tumours with variations of ALK such as an EML4-ALK[3]. ALK inhibitor 2 is a chemical analogue of LDK378 that is a potent ALK inhibitor[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.65mL

1.93mL

0.97mL

19.30mL

3.86mL

1.93mL

参考文献

[1]US20130096100

[2]Lin JJ, Riely GJ, Shaw AT. Targeting ALK: Precision Medicine Takes on Drug Resistance. Cancer Discov. 2017 Feb;7(2):137-155. doi: 10.1158/2159-8290.CD-16-1123. Epub 2017 Jan 25. PMID: 28122866; PMCID: PMC5296241.

[3]Palmer RH, Vernersson E, Grabbe C, Hallberg B. Anaplastic lymphoma kinase: signalling in development and disease. Biochem J. 2009 May 27;420(3):345-61. doi: 10.1042/BJ20090387. PMID: 19459784; PMCID: PMC2708929.

[4]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. PMID: 23742252.