DT2216, utilizing PROTAC technology, is a potent and selective degrader of BCL-XL, a member of the Bcl-2 family. It effectively degrades BCL-XL protein by engaging the Von Hippel-Lindau (VHL) E3 ubiquitin ligase. DT2216 targets various leukemia and cancer cells dependent on BCL-XL while being significantly less harmful to platelets[1].
体内研究
DT2216 (i.p.; 7.5, 15 mg/kg; weekly for 60 days) shows that the 15 mg/kg dosage is more effective in inhibiting the growth of MOLT-4 T-ALL xenografts in mice compared to the 7.5 mg/kg dosage[1].
体外研究
DT2216 (62.5, 125 nM; 72 hours) is lethal to MOLT-4 cells[1].
DT2216 (0.001-10 μM; 72 hour) is highly toxic to MOLT-4 cells, exhibiting an EC50 of 0.052 μM[1].
DT2216 (0.1, 0.3 μM; 24 hours) induces caspase-3-mediated apoptosis in MOLT-4 cells, relying on the involvement of BCL-2 homologous antagonist killer (BAK) and BCL-2-associated X protein (BAX)[1].
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