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Chemical Structure : DT2216
CAS No.: 2365172-42-3
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.
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|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $378 | In stock | |
| 25 mg | $598 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 1542.36 | |
| Formula | C77H96ClF3N10O10S4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2S,4R)-1-((S)-2-(7-(4-((R)-3-((4-(N-(4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-((trifluoromethyl)sulfonyl)phenyl)amino)-4-(phenylthio)butyl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
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1. Khan S, et al. Nat Med. 2019 Dec;25(12):1938-1947.
2. Cancer Discov. 2020 Feb;10(2):174.
3. Thummuri D, et al. Mol Cancer Ther. 2022 Jan;21(1):184-192.
4. He Y, et al. J Hematol Oncol. 2020 Jul 16;13(1):95.
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