JI-101-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJI-101Cat.No.:HY-16265CASNo.:900573-88-8分⼦式:C₂₂H₂₀BrN₅O₂分⼦量:466.33作⽤靶点:EphrinReceptor;PDGFR;VEGFR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(214.44mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1444mL10.7220mL21.4440mL5mM0.4289mL2.1444mL4.2888mL10mM0.2144mL1.0722mL2.1444mL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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.36mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.36mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.36mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JI-101有⼝服活性的有抗癌活性的多靶点激酶抑制剂，可抑制VEGFR2，PDGFRβ和EphB4。IC50&TargetVEGFR2PDGFRβ体外研究JI-101isfoundtobestableinallpreclinicalandhumanlivermicrosomes.The%metabolizedisrangedbetween3.03-3.95acrossthetestedspecieslivermicrosomes.The%metabolizedisrelativelyhigherinmicelivermicrosomesfollowedbydog,humanandratlivermicrosomes[1].体内研究JI-101excretedthroughbilealongwithitsmono-anddi-hydroxymetabolites.Followingoraladministration,JI-101israpidlyabsorbed,reachingCmaxwithin2ꢀh.Thet1/2ofJI-101withintravenousandoralrouteisfoundtobe1.75±0.79and2.66±0.13ꢀh,respectively.TheClandVdbyintravenousrouteforJI-101arefoundtobe13.0±2.62ꢀmL/min/kgand2.11±1.42ꢀL/kg,respectively.ThetissuedistributionofJI-101isextensivewithrapidandpreferreduptakeintolungtissue.Overall,theoralbioavailabilityofJI-101is55%andtheprimaryrouteofeliminationforJI-101isfeces[1].PROTOCOLAnimalRats:PharmacokineticsandbioavailabilityassessmentofJI-101areevaluatedinapreliminaryparallel-groupAdministration[1]studyinmaleS.D.rats.Fourrats(195–210g)perroutereceiveJI-101atadoseof3and30mg/kgfori.v.(viatailvein)andoraldose(bygavage),respectively.Serialbloodsamples(100μL)arecollectedfromretro-orbitalplexusatpre-dose,0.12(i.v.only)0.25,0.5,1,2,4,8,10(oralonly)and24h.BloodsamplesarecollectedintubescontainingK2EDTAastheanticoagulantandcentrifugedfor5minmaintainedat4°Cforplasmaseparationandstoredfrozenat−80±10°Cuntilanalysis[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].GuravSD,etal.Pharmacokinetics,tissuedistributionandidentificationofputativemetabolitesofJI-101-anoveltriplekinaseinhibitorinrats.Arzneimittelforschung.2012Jan;62(1):27-34.McePdfHeightCaution:Producthasnotbeenfullyvalid