BI-9564 , 2mMinDMSO , 1883429-22-8
Synonym(s):
4-(4-Dimethylaminomethyl-2,5-dimethoxy-phenyl)-2-methyl-2H-[2,7]naphthyridin-1-one;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-2,7-naphthyridin-1-one;GTPL8950
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB168.80 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| storage temp. | Store at -20°C |
| solubility | ≥8.82 mg/mL in DMSO with ultrasonic,≥8.32 mg/mL in EtOH with ultrasonic,insoluble in H2O |
| form | crystalline solid |
| color | White to off-white |
Description and Uses
BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (Kds = 14.1 and 239 nM; IC50s = 75 nM and 3.4 μM, respectively) that demonstrates cellular activity by semi-quantitative FRAP assay with ~90% inhibition of BRD9 and BRD7 at 0.1 μM and 1 μM, respectively. It does not bind to other bromodomain-containing BET family members (IC50s >100 μM as assessed by AlphaScreen), kinases, or G protein-coupled receptors and shows off-target selectivity only to the CECR2 bromodomain in in vitro ITC assays (Kd = 258 nM), but not in cell-based assays at concentrations up to 1 μM. BI-9564 has been shown to inhibit the growth of EOL-1 AML cells both in vitro (EC50 = 800 nM) and in a disseminated mouse model of AML (180 mg/kg/day). See the Structural Genomics Consortium (SGC) website for more information.
BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains. It also exhibits antitumor activity in AML xenograft model. BI 9564 can be used as an epigentic probe to study bromodomain biology.
Safety
| Symbol(GHS) |  GHS06 |
| Signal word | Danger |
| Hazard statements | H301 |
| Precautionary statements | P301+P310+P330 |
