BMS-509744 _ITK 抑制剂 - 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作靶点: Itk作通路: Protein Tyrosine Kinase/RTK储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 21.9 mg/mL (35.11 mM; Need ultraso

2、nic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BMS-509744是有效、选择性的、ATP竞争性的 Itk 激酶抑制剂，IC50值为 19 nM。IC50 & Target IC5

3、0: 19 nM (Itk) 1体外研究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 您边的抑制剂师www.MedChemEexhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itkkinase domain 1.体内研究 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.户使本产品发表的科研献 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