Name | (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-(pheny |
Synonyms | DT2216 DT-2216 (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-(pheny |
CAS | 2365172-42-3 |
Molecular Formula | C77H96ClF3N10O10S4 |
Molar Mass | 1542.36 |
Density | 1.39±0.1 g/cm3(Predicted) |
Solubility | Soluble in DMSO |
pKa | 4.60±0.10(Predicted) |
Storage Condition | -20℃ |
Use | 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 |
Reference Show more | 1. Khan S, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 0.648 ml | 3.242 ml | 6.484 ml |
5 mM | 0.13 ml | 0.648 ml | 1.297 ml |
10 mM | 0.065 ml | 0.324 ml | 0.648 ml |
5 mM | 0.013 ml | 0.065 ml | 0.13 ml |
biological activity | DT2216 is a BCL-XL and powerful selective degrading agent based on PROTAC technology. DT2216 inhibits various BCL-XL-dependent leukemia and cancer cells, but is less toxic to platelets. |
target | TargetValue BCL-XL () |
Target | Value |