Tirbanibulin-Mesylate-KX2-391-Mesylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETirbanibulinMesylateCat.No.:HY-10340BCASNo.:1080645-95-9Synonyms:KX2-391Mesylate;KX01Mesylate分⼦式:C₂₇H₃₃N₃O₆S分⼦量:527.63作⽤靶点:Src;Microtubule/Tubulin作⽤通路:ProteinTyrosineKinase/RTK;CellCycle/DNADamage;Cytoskeleton储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:100mg/mL(189.53mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8953mL9.4763mL18.9527mL5mM0.3791mL1.8953mL3.7905mL10mM0.1895mL0.9476mL1.8953mL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(protectfromlight,storedundernitrogen)。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(4.74mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.74mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.74mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性TirbanibulinMesylate(KX2-391Mesylate)⼀种有效的Src抑制剂，在肿瘤细胞中，GI50值为9-60nM。IC50&TargetGI50:9nM(Src,inHuH7cells),13nM(Src,inPLC/PRF/5cells),26nM(Src,inHep3Bcells),60nM(Src,inHepG2cells)[1]体外研究TirbanibulinMesylate(KX2-391Mesylate)isaSrcinhibitorthatisdirectedtotheSrcsubstratepocket.Tirbanibulin(KX2-391)showssteepdose-responsecurvesagainstHuh7(GI50=9nM),PLC/PRF/5(GI50=13nM),Hep3B(GI50=26nM),andHepG2(GI50=60nM),fourhepaticcellcancer(HCC)celllines[1].TirbanibulinMesylate(KX2-391Mesylate)isfoundtoinhibitcertainleukemiacellsthatareresistanttocurrentcommerciallyavailabledrugs,suchasthosederivedfromchronicleukemiacellswiththeT3151mutation.TirbanibulinMesylate(KX2-391Mesylate)isevaluatedinengineeredSrcdrivencellgrowthassaysinNIH3T3/c-Src527FandSYF/c-Src527FcellsandexhibitsGI50with23nMand39nM,respectively[2].体内研究OrallyadministeredTirbanibulinMesylate(KX2-391Mesylate)isshowntoinhibitprimarytumorgrowthandtosuppressmetastasis,inpre-clinicalanimalmodelsofcancer[2].PROTOCOLCellAssay[1]LivercelllinesincludingHuh7,PLC/PRF/5,Hep3B,andHepG2areroutinelyculturedandmaintainedinbasalmediumcontaining2%fetalbovineserum(FBS)at37°Cand5%CO2.Cellsareseededat4.0×103/190μLand8.0×103/190μLperwellof96-wellplateinbasalmediumcontaining1.5%FBS.Theseareculturedovernightat37°Cand5%CO2priortotheadditionofTirbanibulin(KX2-391),atconcentrationsrangingfrom6,564to0.012nMintriplicates.Treatedcellsareincubatedfor3days.TenμLsof3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazoliumbromide(MTT)solution(5mg/mL)isthenaddedtoeachwellonday3andcellsincubatedfor4hours.Theformazanproductisdissolvedwith10%SDSindiluteHCl.Opticaldensityat570nmismeasured.Forcomparisonofactivityandpotency,parallelexperimentsareperformedusingTirbanibulin(KX2-391).Growthinhibitioncurves,50%inhibitionconcentration(GI50),and80%inhibitionconcentration(GI80)aredeterminedusingGraphPadPrism5statisticalsoftware.Dataarenormalizedtorepresentpercentageofmaximumresponseaswellasreportedinopticaldensityatwavelengthof570nm(OD570)signalformat.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•JBiolChem.2019Nov29;294(48):18099-18108.•BrainRes.2020Jun1;1736:146782.•HarvardMedicalSchoolLINCSLIBRARYSeemorecustomervalidationsonwww.MedChemEREFERENCES[1].LauGM,etal.ExpressionofSrcandFAKinhepatocellularcarcinomaandtheeffectofSrcinhibitorsonhepatocellularcarcinomainvitro.DigDisSci,2009,54(7),1465-1474.[2].Fallah-TaftiA,etal.ThiazolylN-benzyl-substitutedacetamidederivatives:synthesis,Srckinaseinhibitoryandanticanceractivities.EurJMedChem,2011,46(1