BI-9564 , ≥98% , 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 |
5mg | RMB446.40 | In Stock |
|
10mg | RMB879.20 | In Stock |
|
25mg | RMB2159.20 | In Stock |
|
50mg | RMB4223.20 | In Stock |
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100mg | RMB5879.20 | 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 |