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5mg |
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25mg |
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50mg |
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Purity: ≥98%
BI-7273 is a novel, potent, selective, and cell-permeable BRD9 inhibitor with IC50 and Kd of 19 and 0.75 nM, respectively; it also shows high effect on BRD7 with IC50 and Kd of 117 nM and 0.3 nM, respectively. BI-7273 may be useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases.
ln Vitro |
having an IC50 and Kd of 19 and 0.75 nM, respectively, BI-7273 is a cell-permeable, selective inhibitor of BRD9. It also exhibits strong effects on BRD7, having an IC50 and Kd of 117 nM and 0.3 nM, respectively. With Kds of 8.8 nM, 210 nM, 2600 nM, and 8600 nM, respectively, BI-7273 is also marginally active against a set of kinases that includes CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2), and TAF1L(2). 1000 nM, 1200 nM, 850 nM, and 10,000 nM. The U2OS cell line exhibits activity with 1 μM of BI-7273. With an EC50 of 1400 nM, BI-7273 inhibits the growth of EOL-1 cells[1].
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References |
[1]. Laetitia J Martin, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.
[2]. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75 |
Molecular Formula |
C20H23N3O3
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Molecular Weight |
353.4149
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CAS # |
1883429-21-7
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Related CAS # |
1883429-21-7; 2305379-66-0 (BRD7-IN-1 free base)
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C(OC)=C2)C3=CC=NC=C13
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InChi Key |
RBUYFHLQNPJMQM-UHFFFAOYSA-N
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InChi Code |
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
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Chemical Name |
4-(4-((dimethylamino)methyl)-3,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
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Synonyms |
BI-7273; BI 7273; BI7273.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~10 mg/mL (~28.30 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (2.83 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.