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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 (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.

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

China 52 United Kingdom 1 United States 10 USA 1 Global 64
Musechem
Tel
+1-800-259-7612
Fax
+1-800-259-7612
Email
info@musechem.com
Country
United States
ProdList
4660
Advantage
60
TargetMol Chemicals Inc.
Tel
+1-781-999-5354 +1-00000000000
Email
marketing@targetmol.com
Country
United States
ProdList
32165
Advantage
58
InvivoChem
Tel
+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
ProdList
6391
Advantage
58
Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
Advantage
58
Aladdin Scientific
Tel
+1-+1(833)-552-7181
Email
sales@aladdinsci.com
Country
United States
ProdList
57505
Advantage
58
TargetMol Chemicals Inc.
Tel
Email
support@targetmol.com
Country
United States
ProdList
38632
Advantage
58
United States Biological
Tel
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Fax
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Email
sales@advtechind.com
Country
United States
ProdList
6075
Advantage
58
ApexBio Technology
Tel
--
Fax
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Email
sales@apexbt.com
Country
United States
ProdList
6251
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58
Cayman Chemical Company
Tel
--
Fax
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Email
cayman@caymanchem.com
Country
United States
ProdList
6213
Advantage
81
United States Biological
Tel
--
Fax
--
Email
chemicals@usbio.net
Country
United States
ProdList
6214
Advantage
80

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

CCT 244747 6-amino-1,3-dimethyl-4-(4-(trifluoromethyl)phenyl)-1,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile 1-[2-CHLORO-6-[[(3-IODOPHENYL)METHYL]AMINO]-9H-PURIN-9-YL]-1-DEOXY-N-METHYL-BETA-D-RIBOFURANURONAMIDE Naquotinib (mesylate) HS-173 BenzaMide, 4-[[2-[3,5-bis(trifluoroMethyl)phenyl]-4,5-bis(4-Methoxyphenyl)-1H-iMidazol-1-yl]Methyl]- (R)-N- (4-(chlorodifluoromethoxy)phenyl)- 6-(3- hydroxypyrrolidin-1- yl)-5- (1H-pyrazol- 5-yl)nicotinamide 4-Propylphenol

  • 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