BMS-509744

Modify Date: 2024-01-02 18:19:51

BMS-509744 Structure
BMS-509744 structure
Common Name BMS-509744
CAS Number 439575-02-7 Molecular Weight 623.829
Density 1.3±0.1 g/cm3 Boiling Point N/A
Molecular Formula C32H41N5O4S2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of BMS-509744


BMS-509744 is a potent and selective Itk inhibitor with an IC50 of 19 nM.

 Names

Name N-[5-[5-(4-acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenyl]sulfanyl-1,3-thiazol-2-yl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamide
Synonym More Synonyms

 BMS-509744 Biological Activity

Description BMS-509744 is a potent and selective Itk inhibitor with an IC50 of 19 nM.
Related Catalog
Target

IC50: 19 nM (Itk)[1]

In Vitro BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain[1].
In Vivo BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell receptor antibody administered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespective of the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma[1].
Kinase Assay BMS-509744 activity (IC50) is determined by kinase assays. The kinase reactions are performed in the presence of 10 μM GST-SLP-76 and various concentrations of ATP for 10 min using 10 ng of enzyme. The concentrations of BMS-509744
Animal Admin Mice: Balb/c mice are injected subcutaneously with the compounds (BMS-509744 and BMS-488516) or vehicle (H2O:ethanol:Tween 80 ) 90:5:5) 15 min before intravenous administration of anti-CD3 antibody. Serum is collected for the analysis of IL-2 and compound levels at 90 min after anti-CD3 antibody administration. IL-2 is measured by ELISA, and compound levels are measured by mass spectrometry[1].
References

[1]. Lin TA, et al. Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry.?2004 Aug 31;43(34):11056-62.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Molecular Formula C32H41N5O4S2
Molecular Weight 623.829
Exact Mass 623.260010
PSA 157.41000
LogP 4.55
Index of Refraction 1.635
Storage condition 2-8℃

 Synonyms

N-[5-({5-[(4-acetylpiperazin-1-yl)carbonyl]-4-methoxy-2-methylphenyl}sulfanyl)-1,3-thiazol-2-yl]-4-{[(3,3-dimethylbutan-2-yl)amino]methyl}benzamide
Benzamide, N-[5-[[5-[(4-acetyl-1-piperazinyl)carbonyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[[(1,2,2-trimethylpropyl)amino]methyl]-
UNII:5V7VG25953
N-[5-({5-[(4-Acetyl-1-piperazinyl)carbonyl]-4-methoxy-2-methylphenyl}sulfanyl)-1,3-thiazol-2-yl]-4-{[(3,3-dimethyl-2-butanyl)amino]methyl}benzamide
BMS-509744
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