2404604-06-2

2404604-06-2 structure

Name: ITK inhibitor 6
Chemical Name: ITK inhibitor 6
CAS Number: 2404604-06-2
Molecular Formula: C₂₈H₂₄F₂N₄O₂
Molecular Weight: 486.51
Catalog: Signaling Pathways Protein Tyrosine Kinase/RTK Itk
Create Date: 2022-06-26 18:41:22
Modify Date: 2024-01-04 16:54:40
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].

Name	ITK inhibitor 6

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.

Molecular Formula	C₂₈H₂₄F₂N₄O₂
Molecular Weight	486.51