Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]-
- CAS No.
- 2839318-19-1
- Chemical Name:
- Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]-
- Synonyms
- dBRD4-BD1;Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]-
- CBNumber:
- CB112280499
- Molecular Formula:
- C50H53F3N8O9
- Molecular Weight:
- 967
- MDL Number:
- MOL File:
- 2839318-19-1.mol
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]- Properties
| Density | 1.41±0.1 g/cm3(Predicted) |
|---|---|
| pka | 10.68±0.40(Predicted) |
| form | Solid |
| color | White to light yellow |
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]- Chemical Properties,Uses,Production
Description
dBRD4-BD1 is a selective BRD4 bromodomain inhibitor. dBRD4-BD1 can selectively degrade BRD4 (DC50 = 280 nM). Notably, dBRD4-BD1 upregulates BRD2/3, a result not observed with degraders using pan-BET ligands. Designing BRD4 selectivity up front enables analysis of BRD4 biology without wider BET-inhibition and simplifies designing BRD4-selective heterobifunctional molecules, such as degraders with new E3 recruiting ligands or for additional probes beyond degraders.
Uses
dBRD4-BD1 is a selective and durable BRD4 degrader with an DC50 value of 280 nM (Dmax=77%). dBRD4-BD1 upregulates BRD2/3 protein level and shows low cytotoxicity than iBRD4-BD1[1].
References
[1] Divakaran A, et al. Development of an N-Terminal BRD4 Bromodomain-Targeted Degrader. ACS Med Chem Lett. 2022 Sep 29;13(10):1621-1627. DOI:10.1021/acsmedchemlett.2c00300
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]- Preparation Products And Raw materials
Raw materials
Preparation Products
Acetamide, 2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-N-[2-[2-[2-[4-[5-[2-[2-methyl-5-(1-methylethyl)phenoxy]-4-pyrimidinyl]-4-[4-(trifluoromethyl)phenyl]-1H-imidazol-1-yl]-1-piperidinyl]ethoxy]ethoxy]ethyl]- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +17819995354 | marketing@targetmol.com | United States | 19961 | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 0513-66337626 18051384581 | sales@chemhifuture.com | China | 5927 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 29243 | 58 |
| Shanghai Fine Biotech Co.,Ltd | 18221172427 | sale@fine-biotech.com | China | 2735 | 58 |
| Supplier | Advantage |
|---|---|
| TargetMol Chemicals Inc. | 58 |
| Nantong QuanYi Biotechnology Co., Ltd | 58 |
| TargetMol Chemicals Inc. | 58 |
| Shanghai Fine Biotech Co.,Ltd | 58 |





