Glesatinib-hydrochloride-MGCD265-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGlesatinibhydrochlorideCat.No.:HY-19642ACASNo.:1123838-51-6Synonyms:MGCD265hydrochloride分⼦式:C₃₁H₂₈ClF₂N₅O₃S₂分⼦量:656.17作⽤靶点:TAMReceptor;c-Met/HGFR作⽤通路:ProteinTyrosineKinase/RTK储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:50mg/mL(76.20mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5240mL7.6200mL15.2400mL5mM0.3048mL1.5240mL3.0480mL10mM0.1524mL0.7620mL1.5240mL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(sealedstorage,awayfrommoisture)。-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(3.81mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(3.81mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.81mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Glesatinibhydrochloride(MGCD265hydrochloride)⼀种具有⼝服活性的，有效的MET/SMO双抑制剂。Glesatinibhydrochloride⼀种酪氨酸激酶抑制剂，可拮抗⾮⼩细胞肺癌(NSCLC)中P糖蛋⽩介导的多药耐药性(MDR)。体外研究Glesatinibhydrochloride(MGCD265hydrochloride;0.01-5μM;for72hours)resultsinadose-dependentinhibitionofcancercellgrowthandshowsthelowIC50valueof0.08μMonNSCLCH1299cells[1].Glesatinibhydrochloride(0.01,0.1,0.5,1μM)significantlyincreasesbyseveral-foldthepercentageofapoptoticcellsinNSCLCH1299cells[1].GlesatinibhydrochloridehasthecytotoxicitytoP-gpoverexpressingcancercellsKB-C2,SW620/Ad300,HEK293/ABCB1,andtheirparentcellsKB-3-1,SW620,HEK293cellswiththeIC50sfellbetween5and10μM[1].Glesatinibhydrochloride(1,3μM;120mins)increasestheintracellular[3H]-Paclitaxelaccumulationandinhibits[3H]-PaclitaxeleffluxincancercelllinesoverexpressingP-gp[2].Glesatinibhydrochloride(0-40μM)stimulatestheATPaseactivityofP-gptransportersinadose-dependentmanner[2].CellProliferationAssay[1]CellLine:NSCLCH1299cellsConcentration:0.01,0.1,1,2,5μMIncubationTime:For72hoursResult:Resultedinadose-dependentinhibitionofcancercellgrowthandshowedthelowestIC50valueof0.08μM.体内研究Glesatinibhydrochloride(MGCD265hydrochloride;15mg/kg/day;orally;40weeks)causesasignificantdecreaseintumorsize[1].AnimalModel:4−6-weekoldfemalebalb/cathymic(nu/nu)micewithHCC827NSCLCtumorxenografts[1]Dosage:15mg/kgAdministration:Orally;daily;40weeks2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Causedasignificantdecreaseintumorsize.户使⽤本产品发表的科研⽂献•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].MorgilloF,etal.DualMETandSMONegativeModulatorsOvercomeResistancetoEGFRInhibitorsinHumanNonsmallCellLungCancer.JMedChem.2017Sep14;60(17):7447-7458.[2].CuiQ,etal.Glesatinib,ac-MET/SMODualInhibitor,AntagonizesP-glycoproteinMediatedMultidrugResistanceinCancerCells.FrontOncol.2019Apr25;9:313.McePdfHeightCaution:Producthasn