CGI1746 is a potent, selective inhibitor of Bruton's tyrosine kinase (BTK, IC50 = 1.9 nM), a non-receptor tyrosine kinase that is important in B lymphocyte development. It blocks both auto-and trans-phosphorylation of BTK by occupying an SH3 binding pocket in the un-phosphorylated enzyme. CGI1746 prevents B-cell...

Soluble in DMSO or ethanol. CGI1746 was identified as a selective and potent ATP-competitive BTK inhibitor with an IC(50) of 1.9nM. It is specific for BTK, with around 1000-fold selectivity over Tec and Src family kinases. Target: BTK , Kinase Group: PTK , Substrate: Tyrosine

Description: CGI1746 is a potent and highly selective small-molecule Btk inhibitor with IC50 of 1.9 nM. Target: BTK, Autophagy. Smiles: CC1=C(C=CC=C1NC(=O)C2=CC=C(C(C)(C)C)C=C2)C=3N=C(NC4=CC=C(C(=O)N5CCOCC5)C=C4)C(=O)N(C)C3. References: Di Paolo JA, et al. Nat Chem Biol, 2011, 7(1):41-50.