BI-9564

ChemicalBook > CAS DataBase List > BI-9564

Product Name: BI-9564
CAS No.: 1883429-22-8
Chemical Name: BI-9564
Synonyms: BI-9564;CS-2421;BI-9564 (BI 9564;BI-9564 >=97% (HPLC);BI-9564,Inhibitor,Epigenetic Reader Domain,inhibit;4-(4-((Dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one;2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-;4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one
CBNumber: CB43134322
Molecular Formula: C20H23N3O3
Formula Weight: 353.41
MOL File: 1883429-22-8.mol

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BI-9564 Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word: Danger
Hazard statements: H301Toxic if swalloed

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 17897
Product name: BI-9564
Purity: ≥98%
Packaging: 500μg
Price: $32
Updated: 2024/03/01

Cayman Chemical

Product number: 17897
Product name: BI-9564
Purity: ≥98%
Packaging: 1mg
Price: $55
Updated: 2024/03/01

Cayman Chemical

Product number: 17897
Product name: BI-9564
Purity: ≥98%
Packaging: 10mg
Price: $214
Updated: 2024/03/01

Tocris

Product number: 5590
Product name: BI9564
Purity: ≥98%(HPLC)
Packaging: 10
Price: $210
Updated: 2021/12/16

TRC

Product number: B373485
Product name: BI9564
Packaging: 1mg
Price: $110
Updated: 2021/12/16

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BI-9564 Chemical Properties,Usage,Production

Description

BI-9564 is a selective inhibitor of BRD9 and BRD7 bromodomains (K_ds = 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 (K_d = 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.

Uses

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.

in vitro

bi-9564 was identified as a brd9/7 specific inhibitor via fragment-based screening and structure-guided design. bi-9564 was found to be bind to brd9 with a higher affinity than to brd7, and was negative on bet family proteins. in addition, bi-9564 demonstrated in vitro off-target selectivity to cecr2, but not in cells [1].

in vivo

in animal study, bomtac:nmrifoxn1nu mice were given two oral doses daily and the concentration of bi-9564 in plasma was measured. dose-dependent aucs were obtained for bi-9564, achieving exposures that were higher compared to the ec50 level for eol-1 cells. moreover, when the oral treatment with bi-9564 at 180 mg/kg was initiated on day 5 and applied daily with an interruption at day 18 and 19, a significant reduction in tumour growth compared to controls was found on day 18 leading to a median tumour growth inhibition value of 52% [1].

IC 50

75 nm and 3.4 μm for brd9 and brd7 bromodomains, respectively

storage

Store at -20°C

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.

BI-9564 Preparation Products And Raw materials

Raw materials

Preparation Products

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BI-9564 Suppliers

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1883429-22-8, BI-9564Related Search:

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BI-9564

4-[4-[(Dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-1,2-dihydro-2,7-naphthyridin-1-one

BI-9564 (BI 9564

CS-2421

2,7-Naphthyridin-1(2H)-one, 4-[4-[(dimethylamino)methyl]-2,5-dimethoxyphenyl]-2-methyl-

BI-9564 >=97% (HPLC)

BI-9564,Inhibitor,Epigenetic Reader Domain,inhibit

4-(4-((Dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one

1883429-22-8