ITK inhibitor 6

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ITK inhibitor 6 

ITK inhibitor 6 (compound 43) 是一种有效的选择性 ITK 抑制剂,ITK、BTK、JAK3、EGFR、LCK 的 IC50s 分别为 4 nM、133 nM、320 nM、2360 nM、155 nM。ITK inhibitor 6 抑制 PLCγ1 和 ERK1/2 的磷酸化。ITK inhibitor 6 具有抗增殖活性。

ITK inhibitor 6

ITK inhibitor 6 Chemical Structure

CAS No. : 2404604-06-2

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生物活性

ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities[1].

IC50 & Target

IC50: 4 nM (ITK); 133 nM (BTK), 320 nM (JAK3), 2360 nM (EGFR), 155 nM (LCK)[1]

体外研究
(In Vitro)

ITK inhibitor 6 (compound 43) shows antiproliferative activities with GI50s of 5.1, 3.7, 3.4, 5.4, 19 µM for Jurkat, Molt-4, CCRF-CEM, H9, HEK 293 T cells, respectively[1].
ITK inhibitor 6 docks into the ATP-binding site of ITK and BTK[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

486.51

Formula

C28H24F2N4O2

CAS 号

2404604-06-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

参考文献
  • [1]. Wang X, et al. Design, synthesis and structure-activity relationship of indolylindazoles as potent and selective covalent inhibitors of interleukin-2 inducible T-cell kinase (ITK). Eur J Med Chem. 2020 Feb 1;187:111918.

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