Information DT2216 DT2216 is a potent and selective degrader of BCL-XL based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells but considerably less toxic to platelets. Targets BCL-XL In vitro DT2216 is a BCL-XL proteolysis targeting chimera (PROTAC) that targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 is more potent against various BCL-XL-dependent leukemia and cancer cells but significantly less toxic to platelets than ABT263 in vitro because VHL is poorly expressed in platelets. In vivo DT2216 effectively inhibits the growth of several xenograft tumors as a single agent or in combination with other chemotherapeutic agents, without causing significant thrombocytopenia. Cell Research(from reference) Cell lines：MOLT-4, RS4;11, NCI-H146, MDA-MB-231, PC-3, HepG2, SW620, 786-O, WI-38, HEK 293T cells Concentrations：0.1 μM, 0.3 μM Incubation Time：24 h
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DT2216
CAS number：2365172-42-3 molecular formula：C77H96ClF3N10O10S4
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| Chinese alias | - | ||
| English alias | (2S,4R)-1-((S)-2-(7-(4-((R)-3-(4-(N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl)methyl)piperazin-1-yl)benzoyl)sulfamoyl)-2-(trifluoromethylsulfonyl)phenylamino)-4-(phenylthio)butyl)piperazin-1-yl)-7-oxoheptanamido)-3,3-dimethylbutanoyl)-4-hydro | ||
| CAS number | 2365172-42-3 | molecular formula | C77H96ClF3N10O10S4 |
| molecular weight | 1542.36 g/mol | Exact mass | - |
| PSA | 321.000 Ų | logp | 12.800 |
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