KB SRC 4 是一种有效的,高度选择性的 c-Src 抑制剂,Ki 和 Kd 值分别为 44 nM 和 86 nM,在浓度高达 125 μM 时,对 c-Abl 也无作用;KB SRC 4 具有抗肿瘤活性。
KB SRC 4 (Compound 4) is a potent, highly selective c-Src inhibitor, with a K
i
of 44 nM and a K
d
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 (K
d
, 160 nM) and Fgr (K
d
, 240 nM), 8-fold selectivity over c-Yes (K
d
, 720 nM), and >40-fold selectivity over Lyn (K
d
, 3200 nM), Hck (K
d
, 4400 nM), and Fyn (K
d
, >40000 nM). KB SRC 4 inhibits the growth of cancer cell lines, with GI
50
s of 11 μM, 12 μM, 11 μM, 6.0 μM against HT-29, SK-BR-3, MCF7, MDA-MB-453, and NIH-3T3, respectively.