| BI-9564BRD9/7 specific inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
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- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 1883429-22-8 | SDF | Download SDF |
| Chemical Name | 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one | ||
| Canonical SMILES | O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13 | ||
| Formula | C20H23N3O3 | M.Wt | 353.41 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 75 nM and 3.4 μM for BRD9 and BRD7 bromodomains, respectively
BI-9564 is a BRD9/7 specific inhibitor.
BRD7 and BRD9 are two important members of the bromodomain family protein. Both BRD7 and BRD9 have been implicated in chromatin remodeling.
In vitro: BI-9564 was identified as a BRD9/7 specific inhibitor via fragment-based screening and structure-guided design. BI-9564 was found to be bind to BRD9 with a higher affinity than to BRD7, and was negative on BET family proteins. In addition, BI-9564 demonstrated in vitro off-target selectivity to CECR2, but not in cells [1].
In vivo: In animal study, BomTac:NMRIFoxn1nu mice were given two oral doses daily and the concentration of BI-9564 in plasma was measured. Dose-dependent AUCs were obtained for BI-9564, achieving exposures that were higher compared to the EC50 level for EOL-1 cells. Moreover, when the oral treatment with BI-9564 at 180 mg/kg was initiated on day 5 and applied daily with an interruption at day 18 and 19, a significant reduction in tumour growth compared to controls was found on day 18 leading to a median tumour growth inhibition value of 52% [1].
Clinical trial: Up to now, BI-9564 is still in the preclinical development stage.
Reference:[1] 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.
