Catalog No.: PC-38054Not For Human Use, Lab Use Only.
DT2216 (DT-2216) is a specific BCL-XL PROTAC by linking ABT263 to a VHL ligand (VHL-L), induces BCL-XL degradation in MOLT-4 T-ALL cells with DC50 of 63 nM.
DT2216 (DT-2216) is a specific BCL-XL PROTAC by linking ABT263 to a VHL ligand (VHL-L), induces BCL-XL degradation in MOLT-4 T-ALL cells with DC50 of 63 nM.
DT2216 exhibits improved antitumor potency (MOLT-4 cells EC50=52 nM) but reduced platelet toxicity by targeting BCL-XL to the VHL E3 ligase for degradation.
DT2216 degrades BCL-XL in a VHL- and proteasome-dependent manner.
DT2216 demonstrates increased antitumor activity of DT2216 in combination with other BCL-2 family protein inhibitors (ABT199 and S63845) and chemotherapy.
DT2216 sensitizes drug resistant tumor cells to chemotherapy in vivo.
