ChemicalBook > CAS DataBase List > dBRD9

dBRD9

Product Name
dBRD9
CAS No.
2170679-45-3
Chemical Name
dBRD9
Synonyms
dBRD9;DBRD09;dBRD-9|||dBRD 9;dBRD9, 10 mM in DMSO;2-[[2,6-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl-methylamino]-N-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide;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
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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
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Hazard and Precautionary Statements (GHS)

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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.

Uses

dBRD9,a PROTAC, can selective degrades BRD9. dBRD9 improves the bromine domain binding profile and reduces the binding activity of the whole BET family[1].

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.

IC 50

BRD9

References

[1] Remillard D, et al. Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands. Angew Chem Int Ed Engl. 2017 May 15;56(21):5738-5743. DOI:10.1002/anie.201611281

dBRD9 Preparation Products And Raw materials

Raw materials

Preparation Products

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dBRD9 Suppliers

Wuhan Yingnuo Pharmaceutical Technology Co., Ltd.
Tel
+86-027-59232304 15387063101
Email
1276242629@qq.com
Country
China
ProdList
9995
Advantage
58
Changzhou Borl Biotechnology Co.,LTD
Tel
13606124132;13656121842
Email
luyan0021@163.com
Country
China
ProdList
242
Advantage
58
Bide Pharmatech Ltd.
Tel
400-400-164-7117 18317119277
Fax
+86-21-61629029
Email
product02@bidepharm.com
Country
China
ProdList
39999
Advantage
60
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696,15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4827
Advantage
55
ShangHai Angti Biotechnology Co., Ltd.
Tel
13764913901
Fax
-
Email
info@angtibio.com
Country
China
ProdList
4975
Advantage
55
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2992
Advantage
58
Beijing Jin Ming Biotechnology Co., Ltd.
Tel
010-60605840 18892239720
Fax
010-60605840
Email
psaitong@jm-bio.com
Country
China
ProdList
12306
Advantage
58
Shanghai finete Pharmaceutical Co., Ltd.
Tel
021-021-00000000 18221039705
Fax
QQ:17263424
Email
finetechpharm@126.com
Country
China
ProdList
215
Advantage
58
Shanghai Yu Ben Biotechnology Co., Ltd.
Tel
021-61350663 15502154572
Fax
-
Email
1639466865@qq.com
Country
China
ProdList
493
Advantage
58
TargetMol Chemicals Inc.
Tel
+1-781-999-5354; +17819995354
Email
marketing@targetmol.com
Country
United States
ProdList
32467
Advantage
58
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View Lastest Price from dBRD9 manufacturers

Hubei Chuchang Biotech Co., Ltd.
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

2170679-45-3, dBRD9Related Search:


  • dBRD9
  • 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
  • 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]-
  • DBRD09
  • dBRD-9|||dBRD 9
  • 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
  • dBRD9, 10 mM in DMSO
  • 2-[[2,6-dimethoxy-4-(2-methyl-1-oxo-2,7-naphthyridin-4-yl)phenyl]methyl-methylamino]-N-[2-[2-[2-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]ethoxy]ethoxy]ethyl]acetamide
  • 2170679-45-3