| Identification | Back Directory | [Name]
PROTAC BRD4 Degrader-13 | [CAS]
2417370-71-7 | [Synonyms]
PROTAC BRD4 Degrader-13
{[(3R,5S)-1-[(2S)-2-(11-{[8-(3,5-difluoropyridin-2-yl)-4-(methanesulfonylmethyl)-15-methyl-14-oxo-8,12,15-triazatetracyclo[8.6.1.02,?.013,1?]heptadeca-1(16),2,4,6,10,13(17)-hexaen-5-yl]formamido}undecanamido)-3,3-dimethylbutanoyl]-5-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-3-yl]oxy}[({2-[6-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)hexanamido]ethoxy}(hydroxy)phosphoryl)oxy]phosphinic acid | [Molecular Formula]
C68H85F2N11O17P2S2 | [MOL File]
2417370-71-7.mol | [Molecular Weight]
1492.55 |
| Hazard Information | Back Directory | [Uses]
PROTAC BRD4 Degrader-13 (compound 9d) is a von Hippel-Lindau system-based PROTAC BRD4 degrader with a linker that can be coupled to ADC antibodies to form PACs (PROTAC-antibody Conjugates). PROTAC BRD4 Degrader-13 can be coupled to STEAP1 and CLL1 antibodies to degrade BRD4 protein in PC3 prostate cancer cells with DC50 values ??of 0.025 nM and 6.0 nM, respectively[1]. | [References]
[1] Dragovich PS, et, al. Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy. J Med Chem. 2021 Mar 11;64(5):2576-2607. DOI:10.1021/acs.jmedchem.0c01846 |
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