DGY-06-116 (SRC inhibitor 15a) is a potent, selective, covalent Src inhibitor (biochemical IC50=3 nM) that taregrs a P-Loop cysteine (Cys277).
BTK, ABL, and most SFK family members such as HCK, BLK, LCK, and YES1 were the main off-targets as confirmed with low nanomolar biochemical IC50s.
DGY-06-116 demonstrated potent antiproliferative effects in lung and breast cancer cell lines (H1957 GI50=0.3 uM).
DGY-06-116 inhibited p-SRCY416 signaling in both H1975 and HCC827 cells at 1 uM.
DGY-06-116 inhibited p-SRCY416 at 2 and 4 h postdosing in spleen tissue samples from C57B6 mice.
