Orantinib-SU6668-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOrantinibCat.No.:HY-10517CASNo.:252916-29-3Synonyms:SU6668;TSU-68分⼦式:C₁₈H₁₈N₂O₃分⼦量:310.35作⽤靶点:PDGFR;FGFR;VEGFR;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥28mg/mL(90.22mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2222mL16.1108mL32.2217mL5mM0.6444mL3.2222mL6.4443mL10mM0.3222mL1.6111mL3.2222mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥10mg/mL(32.22mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Orantinib(SU6668;TSU-68)多靶点的受体酪氨酸激酶抑制剂，对Flt-1，PDGFRβ和FGFR1的Ki值分别为2.1μM，8nM和1.2μM。IC50&TargetPDGFRβFGFR1Flt-18nM(Ki)1.2μM(Ki)2.1μM(Ki)体外研究Orantinib(SU6668;0.03-10μM)showsinhibitoryactivityagainsttyrosinephosphorylationofKDRinVEGFstimulatedHUVECs,andalsoblocksPDGF-stimulatedPDGFRβtyrosinephosphorylationinNIH-3T3cellsoverexpressingPDGFRβ.Orantinib(≥10μM)inhibitsacidicFGF-inducedphosphorylationoftheFGFR1substrate2.However,Orantinib(upto100μM)hasnoeffectonEGF-stimulatedEGFRtyrosinephosphorylationinNIH-3T3cellsoverexpressingEGFR.Furthermore,OrantinibinhibitsVEGF-drivenandFGF-drivenmitogenesisofHUVECswithmeanIC50of0.34μMand9.6μM,respectively[1].InhumanmyeloidleukemiaMO7Ecells,Orantinib(SU6668)inhibitsthetyrosineautophosphorylationofstemcellfactor(SCF)receptor,c-kit,withIC50of0.1-1μM,aswellasERK1/2phosphorylation.Inaddition,OrantinibsuppressesSCF-inducedproliferationofMO7EcellswithanIC50of0.29μM,andinducesapoptosis[2].体内研究Orantinib(SU6668;75-200mg/kg)causestumorgrowthinhibitiononseveraltumortypesinxenograftmodelsinathymicmice,suchasA375,Colo205,H460,Calu-6,C6,SF763T,andSKOV3TP5cells.Orantinib(75mg/kg)alsoinhibitstumorangiogenesisofC6gliomaxenografts[1].InatumormodelofHT29humancoloncarcinoma,Orantinib(200mg/kg)decreasestheaveragevesselpermeabilityandaveragefractionalplasmavolumeinthetumorrimandcore.Orantinibenhancesabnormalstromaldevelopmentattheperipheryofcarcinomas[3].Moreover,Orantinib(TSU-68;200mg/kg)augmentstheeffectofchemotherapeuticinfusioninarabbitVX2livertumormodel[4].户使⽤本产品发表的科研⽂献•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•PLoSGenet.2022Jun27;18(6):e1010292.•Patent.US20180263995A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LairdAD,etal.SU6668isapotentantiangiogenicandantitumoragentthatinducesregressionofestablishedtumors.CancerRes,2000,60(15),4152-4160.[2].SmolichBD,etal.TheantiangiogenicproteinkinaseinhibitorsSU5416andSU6668inhibittheSCFreceptor(c-kit)inahumanmyeloid2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEleukemiacelllineandinacutemyeloidleukemiablasts.Blood,2001,97(5),1413-1421.[3].MarzolaP,etal.InvivoassessmentofantiangiogenicactivityofSU6668inanexperimentalcoloncarcinomamodel.ClinCancerRes,2004,10(2),739-750.[4].KimHC,etal.AugmentationofchemotherapeuticinfusioneffectbyTSU-68,anoraltargetedantiangiogenicagent,inarabbitVX2livertumormodel.CardiovascInterventRadiol.2012Feb;35(1):168-75McePdfHeightCaution: