SJ11646 is a Dasatinib-based LCK PROTAC degrader with a DC50 of 0.00838 pM. It exhibits potent cytotoxicity against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, significantly prolongs LCK signal inhibition, and induces apoptosis in T-ALL cells. SJ11646 binds with high affinity to 51 human kinases, particularly ABL1, KIT, and DDR1. In mouse models of T-ALL, SJ11646 demonstrates exceptional anti-leukemic efficacy.
