ITK inhibitor 6

Names

[ CAS No. ]:
2404604-06-2

[ Name ]:
ITK inhibitor 6

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Itk

[Target]

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


[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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C28H24F2N4O2

[ Molecular Weight ]:
486.51

Related Compounds