Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBMS-509744Cat.No.:HY-11092CASNo.:439575-02-7分?式:C??H??N?O?S?分?量:623.83作?靶點:Itk作?通路:ProteinTyrosineKinase/RTK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:21.9mg/mL(35.11mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.6030mL8.0150mL16.0300mL5mM0.3206mL1.6030mL3.2060mL10mM0.1603mL0.8015mL1.6030mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.01mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.01mM);ClearsolutionBIOLOGICALACTIVITY?物活性BMS-509744有效、選擇性的、ATP競爭性的Itk激酶抑制劑，IC50值為19nM。IC50&TargetIC50:19nM(Itk)[1]體外研究BMS-509744reducesT-cellreceptor-inducedfunctionsincludingPLCγ1tyrosinephosphorylation,calciummobilization,IL-2secretion,andT-cellproliferationinvitroinbothhumanandmousecells.BMS-488516andBMS-509744potentlyinhibitItkinvitrowithIC50valuesof96and19nM,respectively.BothcompoundsexhibitcompetitivekineticswithrespecttoATP,suggestingthattheybindtotheATPbindingsiteoftheItkkinasedomain[1].體內(nèi)研究BMS-509744andBMS-488516suppresstheproductionofIL-2inducedbyanti-T-cellreceptorantibodyadministeredtomice.BMS-509744exhibitsa50%inhibitorycapacitywhendosedat50mg/kg,irrespectiveoftheamountofinductionantibody.BMS-509744alsosignificantlydiminisheslunginflammationinamousemodelofovalbumin-inducedallergy/asthma[1].PROTOCOLKinaseAssay[1]BMS-509744activity(IC50)isdeterminedbykinaseassays.Thekinasereactionsareperformedinthepresenceof10μMGST-SLP-76andvariousconcentrationsofATPfor10minusing10ngofenzyme.TheconcentrationsofBMS-509744MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Balb/cmiceareinjectedsubcutaneouslywiththecompounds(BMS-509744andBMS-488516)orAdministration[1]vehicle(H2O:ethanol:Tween80)90:5:5)15minbeforeintravenousadministrationofanti-CD3antibody.SerumiscollectedfortheanalysisofIL-2andcompoundlevelsat90minafteranti-CD3antibodyadministration.IL-2ismeasuredbyELISA,andcompoundlevelsaremeasuredbymassspectrometry[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?ProcNatlAcadSciUSA.2022Oct25;119(43):e2207280119.?CancerCellInt.2019Feb14;19:32.?CancerCellInt.2019Feb14;19:32.?HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].LinTA,etal.SelectiveItkinhibitorsblockT-cellactivationandmurinelunginflammation.Biochemistry.?2004Aug31;43(34):11056-62.McePdfHeightCaution:Producthasnotbeenfu