dBRD9
- Product Name
- dBRD9
- CAS No.
- 2170679-45-3
- Chemical Name
- dBRD9
- Synonyms
- dBRD9;DBRD09;dBRD-9|||dBRD 9;2-((2,6-Dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)benzyl)(methyl)amino)-N-(2-(2-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethoxy)ethoxy)ethyl)acetamide;2-({[2,6-dimethoxy-4-(2-methyl-1-oxo-1,2-dihydro-2,7-naphthyridin-4-yl)phenyl]methyl}(methyl)amino)-N-{2-[2-(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethoxy)ethoxy]ethyl}acetamide;Acetamide, 2-[[[4-(1,2-dihydro-2-methyl-1-oxo-2,7-naphthyridin-4-yl)-2,6-dimethoxyphenyl]methyl]methylamino]-N-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethyl]-
- CBNumber
- CB74667813
- Molecular Formula
- C40H45N7O10
- Formula Weight
- 783.84
- MOL File
- 2170679-45-3.mol
dBRD9 Property
- Boiling point:
- 1014.2±65.0 °C(Predicted)
- Density
- 1.357±0.06 g/cm3(Predicted)
- pka
- 10.74±0.40(Predicted)
- form
- Solid
- color
- Light yellow to yellow
- InChIKey
- AIOCFZJGGGEWDK-UHFFFAOYSA-N
- SMILES
- O=C1N(C2CCC(=O)NC2=O)C(=O)C2=CC=CC(NCCOCCOCCNC(=O)CN(C)CC3C(=CC(C4=CN(C)C(=O)C5=CN=CC=C45)=CC=3OC)OC)=C12
dBRD9 Chemical Properties,Usage,Production
Description
dBRD9 is a potent and selective Degrader (PROTAC?) of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). dBRD9 is composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide. Does not degrade BRD4 or BRD7 at concentrations up to 5 μM. Displays antiproliferative effects in human AML cell lines.
Biological Activity
dBRD9 is a PEG-linked pomalidomide conjugate and was found to prompt rapid BRD9 degradation over a broad range of concentrations. Besides, also shows an improved bromodomain engagement profile, with reduced binding activity across the BET family. Meanwhile, dBRD9 (0.5, 5, 50, 500, 5000 nM; 4 h) decreases the expression of BRD9 protein in MOLM-13 cells in a dose-dependent manner. However, it shows no significant effect on the expression of BRD4 and BRD7 proteins. Moreover, dBRD9 (100 nM; 2 h) shows selectivity for BRD9 degradation with a 5.5 median fold lower abundance in dBRD9 treated samples in MOLM-13 cells. However, the levels of other proteins were remarkably static between treatments, with 99% of proteins differing less than 0.30 fold. In addition, dBRD9 (0-100; 7 days) shows a potent anti-proliferative effect in EOL-1 and MOML-13 cells in a dose-dependent manner. All in all, dBRD9 is a PROTAC and can selectively degrade BRD9.
dBRD9 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from dBRD9 manufacturers
- Product
- dBRD9 2170679-45-3
- Price
- US $0.00-0.00/MG
- Min. Order
- 1MG
- Purity
- 98
- Supply Ability
- 100G
- Release date
- 2024-04-17