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dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM, and has antitumor activity. IC50 & Target: IC50: 14 nM (BET) In Vitro: dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4. In Vivo: dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL.
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