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BI-9564, BRD9 Bromodomain Inhibitor

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BI-9564, BRD9 Bromodomain Inhibitor

$129.00
A potent, selective and cell-permeable BRD9 inhibitor.
Catalog No. Unit Price Qty
M60323-2s 2 mg solid $129.00

Details

Product Information
Molecular Weight: 353.42
Formula: C20H23N3O3
Purity: ≥98%
CAS#: 1883429-22-8
Solubility: DMSO up to 100 mM
Chemical Name: 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

BI-9546 is a potent, selective and cell-permeable BRD9 inhibitor with IC50 ~75 nM (Alpha assay). It has good selectivity over BRD7 (IC50 ~3410 nM, Alpha assay). It has high selectivity against the other bromodomain family members (48 bromodomains) and kinases. In EOL-1 cellular proliferation assay, BI-9546 has IC50 at 800 nM. It has very good pharmacokinetic profiling, and also displays antitumor activity in EOL-1 AML xenograft model with oral treatment. BI-9546 could be a useful chemical tool to further explore BRD9 bromodomain biology in both in vitro and in vivo settings.

How to Use:

In vitro: BI-9546 was used at 1-10 µM in vitro and cellular assays.
In vivo: BI-9546 was orally dosed to mice in EOL-1 AML xenograft model at 180 mg/kg once per day.


Reference:

  1. 1. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. (2016) J Med Chem. 59(10):4462-75. 


BI-9546_spec.pdf 
BI-9546_MSDS.pdf     

Products are for research use only. Not for human use. 

Description

Details

Product Information
Molecular Weight: 353.42
Formula: C20H23N3O3
Purity: ≥98%
CAS#: 1883429-22-8
Solubility: DMSO up to 100 mM
Chemical Name: 4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

Biological Activity:

BI-9546 is a potent, selective and cell-permeable BRD9 inhibitor with IC50 ~75 nM (Alpha assay). It has good selectivity over BRD7 (IC50 ~3410 nM, Alpha assay). It has high selectivity against the other bromodomain family members (48 bromodomains) and kinases. In EOL-1 cellular proliferation assay, BI-9546 has IC50 at 800 nM. It has very good pharmacokinetic profiling, and also displays antitumor activity in EOL-1 AML xenograft model with oral treatment. BI-9546 could be a useful chemical tool to further explore BRD9 bromodomain biology in both in vitro and in vivo settings.

How to Use:

In vitro: BI-9546 was used at 1-10 µM in vitro and cellular assays.
In vivo: BI-9546 was orally dosed to mice in EOL-1 AML xenograft model at 180 mg/kg once per day.


Reference:

  1. 1. Martin LJ, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. (2016) J Med Chem. 59(10):4462-75. 


BI-9546_spec.pdf 
BI-9546_MSDS.pdf     

Products are for research use only. Not for human use. 

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