ITK inhibitor 6

Modify Date: 2024-01-04 16:54:40

ITK inhibitor 6 Structure
ITK inhibitor 6 structure
Common Name ITK inhibitor 6
CAS Number 2404604-06-2 Molecular Weight 486.51
Density N/A Boiling Point N/A
Molecular Formula C28H24F2N4O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of 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].

 Names

Name ITK inhibitor 6

 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
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