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BI-7273 - CAS 1883429-21-7

Inquiry

BI-7273 is a potent BRD9 bromodomain inhibitor (Ki = 15.4 nM; IC50 = 19 nM). BI-7273 structurally related BRD7 bromodomain (IC50 = 117 nM) without effect against the BRD2 and BRD4 bromodomain or a panel of kinases. BI-7273 has potential for use in treating acute myeloid leukemia according to a study in vitro (EC50 = 1.4 µM).

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Molecular Formula

C20H23N3O3

Molecular Weight

353.41

BI-7273

- Specification
  - Purity
    
    >98%
    
    Solubility
    
    Soluble in DMSO, Ethanol
    
    Appearance
    
    Crystalline Solid
    
    Application
    
    A potent BRD9 bromodomain inhibitor for the treatment of leukemia.
    
    Shelf Life
    
    2 years
    
    Storage
    
    Store at 2-8°C for short term (days to weeks) or -20°C for long term (months to years)
    
    IUPAC Name
    
    4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one
    
    Synonyms
    
    4-{4-[(dimethylamino)methyl]-2,6-dimethoxyphenyl}-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one; 4-(4-((Dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one; 2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-3,5-dimethoxyphenyl]-2-methyl-; BI7273; BI 7273
- Properties
  - Boiling Point
    
    528.1±50.0 °C at 760 mmHg
    
    Density
    
    1.2±0.1 g/cm3
    
    InChI Key
    
    RBUYFHLQNPJMQM-UHFFFAOYSA-N
    
    InChI
    
    InChI=1S/C20H23N3O3/c1-22(2)11-17-18(25-4)8-13(9-19(17)26-5)16-12-23(3)20(24)15-10-21-7-6-14(15)16/h6-10,12H,11H2,1-5H3
    
    Canonical SMILES
    
    CN1C=C(C2=C(C1=O)C=NC=C2)C3=CC(=C(C(=C3)OC)CN(C)C)OC
- Reference Reading
  - 1.Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor.
    
    Martin LJ;Koegl M;Bader G;Cockcroft XL;Fedorov O;Fiegen D;Gerstberger T;Hofmann MH;Hohmann AF;Kessler D;Knapp S;Knesl P;Kornigg S;Müller S;Nar H;Rogers C;Rumpel K;Schaaf O;Steurer S;Tallant C;Vakoc CR;Zeeb M;Zoephel A;Pearson M;Boehmelt G;McConnell D J Med Chem. 2016 May 26;59(10):4462-75. doi: 10.1021/acs.jmedchem.5b01865. Epub 2016 Mar 10.
    
    Components of the chromatin remodelling switch/sucrose nonfermentable (SWI/SNF) complex are recurrently mutated in tumors, suggesting that altering the activity of the complex plays a role in oncogenesis. However, the role that the individual subunits play in this process is not clear. We set out to develop an inhibitor compound targeting the bromodomain of BRD9 in order to evaluate its function within the SWI/SNF complex. Here, we present the discovery and development of a potent and selective BRD9 bromodomain inhibitor series based on a new pyridinone-like scaffold. Crystallographic information on the inhibitors bound to BRD9 guided their development with respect to potency for BRD9 and selectivity against BRD4. These compounds modulate BRD9 bromodomain cellular function and display antitumor activity in an AML xenograft model. Two chemical probes, BI-7273 (1) and BI-9564 (2), were identified that should prove to be useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings.
- Preparing Stock Solutions
  - ConcentrationVolumeMass 1 mg 5 mg 10 mg
    
    1 mM 2.8296 mL 14.1479 mL 28.2957 mL
    
    5 mM 0.5659 mL 2.8296 mL 5.6591 mL
    
    10 mM 0.2830 mL 1.4148 mL 2.8296 mL
    
    50 mM 0.0566 mL 0.2830 mL 0.5659 mL

ConcentrationVolumeMass	1 mg	5 mg	10 mg
1 mM	2.8296 mL	14.1479 mL	28.2957 mL
5 mM	0.5659 mL	2.8296 mL	5.6591 mL
10 mM	0.2830 mL	1.4148 mL	2.8296 mL
50 mM	0.0566 mL	0.2830 mL	0.5659 mL

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