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4000-520-616 / 18915418616
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0512-67156496
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商品描述
BI-9564
- Catalog No.：MC1262
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1883429-22-8
- MolecularFormula：
- C20H23N3O3
- Purity：
- >98%
- Target：
- Epigenetic Reader Domain
- IC50：
- Kd: 20 nM (BRD9)
- In Vitro：
- BI-9564 (<5 μm)="" shows="" no="" activity="" against="" 324="" kinases,="" and="" at="" 10="" μm,="" 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[1]. BI-9564 shows Kd of 73 nM for BRD7, and is >10-fold more selective for BRD9 over the highly homologues bromodomain BRD7, which has been implied as a tumor suppressor and is down-regulated in cancer cells[2].
- In Vivo：
- BI-9564 (180 mg/kg, p.o.) shows attractive ADME/PK profiles for in vivo proof-of-concept studies. BI-9564 results in a modest but significant additional survival benefit of 2 days compared to survival of the control group in a xenograft model of human AML[1].
- Fields：
- BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
- Specificity：
- Target:Epigenetic Reader Domain. Fields: BI-9564 is a selective, and cell-permeable BRD9 BD inhibitor, with Kd of 5.9 nM for BRD9, and IC50 of > 100 μM for BET family.
- Source：
- Rabbit
- Dilution：
- Kd: 20 nM (BRD9)
- Concentration：
- >98%
- Other Name：
- BI9564,BI 9564
- MolecularWeight(Da)：
- 353.41
- 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.
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