ITK inhibitor 6 

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

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

486.51

C₂₈H₂₄F₂N₄O₂

2404604-06-2

Room temperature in continental US; may vary elsewhere.

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

• [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.  [Content Brief]