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DT2216 is a selective B-cell lymphoma extra large (BCL-XL) proteolysis-targeting chimera (PROTAC). DT2216 targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets.
In vivo, DT2216 (i.p.; weekly for 60 days) of 15 mg/kg is more effective at suppressing the growth of MOLT-4 T-ALL xenografts in mice than 7.5 mg/kg.
Cell Death Dis. 2025 Mar 20;16(1):194.
Novel selective strategies targeting the BCL-2 family to enhance clinical efficacy in ALK-rearranged non-small cell lung cancer
DT2216 purchased from AbMole
Cell Death Differ. 2024 Dec 03.
HRK downregulation and augmented BCL-xL binding to BAK confer apoptotic protection to therapy-induced senescent melanoma cells
DT2216 purchased from AbMole
| Molecular Weight | 1542.36 |
| Formula | C77H96ClF3N10O10S4 |
| CAS Number | 2365172-42-3 |
| Solubility (25°C) | DMSO 20 mg/mL |
| Storage | -20°C, sealed |
[1] Cancer Discov. The PROTAC DT2216 Targets Cancer by Promoting BCL-X L Degradation
| Related PROTAC Products |
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| CR8
CR8 is a potent and selective inhibitor of cyclin dependent kinase (CDK1, 2, 5, 7, and 9). |
| Indisulam
Indisulam is a carbonic anhydrase inibitor and antitumor CDK inhibitor. Indisulam targets the G1 phase of the cell cycle by depleting cyclin E. inducing p53 and p21, and inhibiting CDK2, causing a blockade in the G1/S transition. |
| dBET6
dBET6 is a highly potent, selective and cell-permeable PROTAC connected by ligands for Cereblon and BET, with an IC50 of 14 nM, and has antitumor activity. |
| A1874
A1874 is a BRD4-degrading PROTAC which inhibits many cancer cell lines proliferation, with DC50 of 32 nM (induce BRD4 degradation in cells). |
| MZ 1
MZ 1 is a PROTAC BRD4 degrader, with Kd values of 382/120, 119/115, and 307/228 nM for BRD4 BD1/2, BRD3 BD1/2, and BRD2 BD1/2, respectively. |
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