Lck-Inhibitor-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELckInhibitorCat.No.:HY-12072CASNo.:847950-09-8分⼦式:C₃₁H₃₀N₈O分⼦量:530.62作⽤靶点:Src作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(188.46mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8846mL9.4229mL18.8459mL5mM0.3769mL1.8846mL3.7692mL10mM0.1885mL0.9423mL1.8846mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(4.71mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LckInhibitor⼀种有效的⼝服活性淋巴细胞特异性激酶(Lck)抑制剂，对Lck，Lyn，Src和Syk激酶的IC50分别为7、2.1、4.2和200nM。与MAPK，CDK和RSK家族代表相⽐，LckInhibitor对Lck的选择性⾼出1000倍以上。LckInhibitor抑制T细胞增殖和关节炎模型。体外研究LckInhibitor(compound25)exhibitsgoodpotencyintheT-cellreceptor-inducedIL-2secretionassay(IL-2,IC50=0.46μM)andalsoinhibitssubsequentT-cellproliferation(T-cellprolif,IC50=0.53μM)inthesamehumanT-cells.LckInhibitoralsoinhibitsahumanmixedlymphocytereaction(huMLR)witha10-foldincreaseinpotencyascomparedtotheotherinvitrocellassaysutilizingpurifiedhumancells.LckInhibitoralsodisplaysinhibitionofamechanism-basedbiochemicalcellassayprobingLck-dependentTCR-chainphosphorylation(TCR-chain).LckInhibitorshowsa10-foldreductioninpotencywhenIL-2isinducedinareceptor-independentfashionbystimulatingwithphorbolesterandcalciumionophore(PMA/iono).LckInhibitorexhibitsasimilarlevelofpotencywhentestedinageneralproliferationassayusingthehumanT-cellline,Jurkat(JKT)[1].体内研究LckInhibitor(0-60mg/kg;p.o.;oncedaily;fromday9today17)showsadose-dependentinhibitionofarthritis[1].LckInhibitor(p.o.;5mg/kg)treatmentshowstheCmax,AUC0-∞,tmaxandF%are82ng/mL,862ngh/mL,and17%,respectively[1].AnimalModel:MaleLewisrat(adjuvant-inducedarthritismodel)[1]Dosage:0,30,and60mg/kgAdministration:P.o.;oncedaily;fromday9today17Result:Showedadose-dependentinhibitionofarthritis,withanED50estimatedat24mg/kg.AnimalModel:Sprague-DawleyRats[1]Dosage:P.o.(PharmacokineticAnalysis)Administration:5mg/kgResult:TheCmax,AUC0-∞,tmaxandF%were82ng/mL,862ngh/mL,and17%,respectively.REFERENCES[1].Martin,MatthewW.;Newcomb,John;Nunes,JosephJ.;etal.Structure-BasedDesignofNovel2-Amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-onesasPotentandOrallyActiveInhibitorsofLymphocyteSpecificKinase(Lck):2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESynthesis,S[2].Liew,ChinY.;Ma,XiaoH.;Liu,Xianghui;Yap,ChunW.SVMModelforVirtualScreeningofLckInhibitors.JournalofChemicalInformationandModeling(2009),49(4),877-885.McePdfHeightCaution:Producthasnotbeenful