KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.
KB SRC 4 (Compound 4) is a potent, highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM. KB SRC 4 is selective between Src family members, with >2-fold selectivity over both Lck (Kd, 160 nM) and Fgr (Kd, 240 nM), 8-fold selectivity over c-Yes (Kd, 720 nM), and >40-fold selectivity over Lyn (Kd, 3200 nM), Hck (Kd, 4400 nM), and Fyn (Kd, >40000 nM). KB SRC 4 inhibits the growth of cancer cell lines, with GI50s of 11 μM, 12 μM, 11 μM, 6.0 μM against HT-29, SK-BR-3, MCF7, MDA-MB-453, and NIH-3T3, respectively[1].
References:
[1]. Brandvold KR, et al. Development of a highly selective c-Src kinase inhibitor. ACS Chem Biol. 2012 Aug 17;7(8):1393-8.