SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia.
SJ11646 is a LCK-targeting PROTAC degrader based on Dasatinib, exhibiting a DC50 of 0.00838 pM. This compound demonstrates potent cytotoxic effects against LCK-activated T-cell acute lymphoblastic leukemia (T-ALL) cells and primary leukemia samples, effectively prolonging LCK signaling suppression and inducing apoptosis in T-ALL. Additionally, SJ11646 binds with high affinity to 51 human kinases, including ABL1, KIT, and DDR1, and shows enhanced antileukemic efficacy in T-ALL mouse models, making it a valuable tool for research into novel therapeutic strategies for leukemia.
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