Tilfrinib (compound 4f) is a potent and selective Brk/PTK6 inhibitor with an IC50 value of 3.15 nM for Brk. Tilfrinib shows good anti-proliferative activity and has potential of anti-tumour[2].IC50 & Target:IC50: 3.15 nM (Brk), PTK6[2].In Vitro:Tilfrinib (20 μM; 36 h) shows inhibition of PTK6, and decreases the ETV4 WT-induced expression of CXCL1 or CXCL8 in UM-UC-3 cells and expression of VEGFA or MMP9 in TANs.
Tilfrinib (compound 4f) shows good anti-proliferative activity against MCF7, HS-578/T and BT-549 cells with GI50 values of 0.99, 1.02 and 1.58 μM[2].