BMS-509744 _ITK 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBMS-509744Cat. No.: HY-11092CAS No.: 439575-02-7分式: CHNOS分量: 623.83作靶點(diǎn): Itk作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 21.9 mg/mL (35.11 mM; Need ultraso

2、nic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.6030 mL 8.0150 mL 16.0300 mL5 mM 0.3206 mL 1.6030 mL 3.2060 mL10 mM 0.1603 mL 0.8015 mL 1.6030 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BMS-509744是有效、選擇性的、ATP競爭性的 Itk 激酶抑制劑，IC50值為 19 nM。IC50 & Target IC5

3、0: 19 nM (Itk) 1體外研究BMS-509744 reduces T-cell receptor-induced functions including PLC1 tyrosine phosphorylation, calciummobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 andBMS-509744 potently inhibit Itk in vitro with IC50 values of 96 and 19

4、 nM, respectively. Both compounds1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEexhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itkkinase domain 1.體內(nèi)研究 BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell recept

5、or antibodyadministered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespectiveof the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mousemodel of ovalbumin-induced allergy/asthma 1.PROTOCOLKinase Assay 1 BMS-509744 a

6、ctivity (IC50) is determined by kinase assays. The kinase reactions are performed in thepresence of 10 M GST-SLP-76 and various concentrations of ATP for 10 min using 10 ng of enzyme. Theconcentrations of BMS-509744MCE has not independently confirmed the accuracy of these methods. They are for refer

7、ence only.Animal Mice: Balb/c mice are injected subcutaneously with the compounds (BMS-509744 and BMS-488516) orAdministration 1 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

8、 min after anti-CD3 antibodyadministration. IL-2 is measured by ELISA, and compound levels are measured by mass spectrometry 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Cancer Cell Int. 2019 Feb 14;19:32. Cancer Cell Int. 2019 Feb 14;1

9、9:32. Harvard Medical School LINCS LIBRARYSee more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Lin TA, et al. Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry.?2004 Aug 31;43(34):11056-62.McePdfHeightCaution: Product has not been fully validated for medical