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Purity: ≥98%
BI-9564 is a novel, cell-permeable, noncytotoxic, potent, and selective inhibitor of BRD9 (bromodomain-containing protein) and BRD7 BD (bromodomains) with Kd values of 14.1 and 239 nM, and IC50 values of 75 nM and 3.4 µM for BRD9/7 respectively. Selective inhibitors of bromodomain-containing protein 9 (BRD9) may have therapeutic potential in the treatment of human malignancies and inflammatory diseases. BI-9564 is useful in further exploring BRD9 bromodomain biology in both in vitro and in vivo settings. BI-9564 (<5 10='' 324='' shows='' no='' activity='' against='' and='' at='' an='' inhibition=''>40% is observed for only 2 out of 55 GPCRs. BI-9564 has antiproliferative effect on human acute myeloid eosinophilic leukemia cell line EOL-1, with EC50 of 800 nM.
| ln Vitro |
BI-9564 (<5 μM) exhibits no activity against 324 kinases, and only 2 out of 55 GPCRs exhibit an inhibition >40% at 10 μM. With an EC50 of 800 nM, BI-9564 exhibits antiproliferative activity on the human acute myeloid eosinophilic leukemia cell line EOL -1[1]. In comparison to the highly homologous bromodomain BRD7, which has been suggested to be a tumor suppressor and is down-regulated in cancer cells, BI-9564 exhibits a Kd of 73 nM for BRD7 and is >10-fold more selective for BRD9[2].
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| ln Vivo |
Attractive ADME/PK profiles are demonstrated by BI-9564 (180 mg/kg, po) for in vivo proof-of-concept investigations. In a xenograft model of human AML, BI-9564 produces a small but significant additional survival benefit of 2 days compared to survival of the control group[1].
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| References |
[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.
[2]. Rezaul M. Karim, et al. An Advanced Tool To Interrogate BRD9. J. Med. Chem., 2016, 59 (10), pp 4459-4461 |
| Molecular Formula |
C20H23N3O3
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| Molecular Weight |
353.41
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| CAS # |
1883429-22-8
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| SMILES |
O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| 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.
J Med Chem. 2016 May 26; 59(10): 4462–4475. |
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Binding mode of the methylpyridopyrimidinone3or dimethylpyridinone4scaffold in BRD9 BD (compound3: PDB code 5F2P; compound4: PDB code 5F25).J Med Chem. 2016 May 26; 59(10): 4462–4475. |
(a–c) Binding mode of BRD9 BD inhibitors (a)11, (b)1, and (c)2[compound11: PDB code 5F1L; compound1:J Med Chem. 2016 May 26; 59(10): 4462–4475. |
ITC analysis of compounds1and2(T= 293.15 K).
1and2block EOL-1 cell proliferation with EC50’s of 1400 and 800 nM, respectively.J Med Chem. 2016 May 26; 59(10): 4462–4475. |
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FRAP assay using U2OS cells transfected with GFP–BRD9
Efficacy and tolerability of BRD9 inhibitor2in a xenograft model of human AML.J Med Chem. 2016 May 26; 59(10): 4462–4475. |
Summary of Properties of1and2.J Med Chem. 2016 May 26; 59(10): 4462–4475. |
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