c-Src Kinase-IN-1

c-Src Kinase-IN-1 (compound 4) potently inhibits purified c-Src kinase with a K_i value of 44 nM, and exhibits no inhibitory activity against purified c-Abl kinase at concentrations up to 125 μM^[1].
c-Src Kinase-IN-1 exhibits high kinome selectivity. At a concentration of 10 μM, over 95% of ligand displacement activity is restricted to c-Src, c-Raf and B-Raf. Moreover, it binds selectively to Src family members relative to c-Src (K_d = 86 nM): it shows over 2-fold selectivity for Lck and Fgr, 8-fold selectivity for Yes, and over 40-fold selectivity for Lyn, Hck and Fyn^[1].
c-Src Kinase-IN-1 inhibits the purified c-Src^TM mutant kinase with a K_i value of 175 nM, indicating that the major P-loop sequence alone does not determine its selectivity^[1].
c-Src Kinase-IN-1 is cell-permeable and inhibits the activity of c-Src in MEF cells expressing full-length c-Src, with an IC₅₀ of 1.9 μM^[1].
c-Src Kinase-IN-1 (72 h) inhibits the growth of HT-29, SK-BR-3, MCF7 and MDA-MB-453 cancer cell lines with GI₅₀ values ranging from 6.0 to 12 μM; it exerts no growth inhibitory effect on the non-cancerous NIH-3T3 cell line even at concentrations as high as 100 μM^[1].
c-Src Kinase-IN-1 (10 μM; 72 h) inhibits the 3D growth of 4T1 metastatic breast cancer cells, and combined use with a c-Abl inhibitor significantly attenuates this inhibitory effect^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.