Sitravatinib-MGCD516-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESitravatinibCat.No.:HY-16961CASNo.:1123837-84-2Synonyms:MGCD516;MG-516分⼦式:C₃₃H₂₉F₂N₅O₄S分⼦量:629.68作⽤靶点:VEGFR;c-Kit;FLT3;DiscoidinDomainReceptor;TrkReceptor作⽤通路:ProteinTyrosineKinase/RTK;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥32mg/mL(50.82mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM1.5881mL7.9405mL15.8811mL5mM0.3176mL1.5881mL3.1762mL10mM0.1588mL0.7941mL1.5881mL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1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE、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(3.97mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(3.97mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(3.97mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.75mg/mL(4.37mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Sitravatinib(MGCD516)⼀种有⼝服活性的受体酪氨酸激酶(RTK)抑制剂。抑制Axl，MER，VEGFR3，VEGFR2，VEGFR1，KIT，FLT3，DDR2，DDR1，TRKA，和TRKB，IC50分别为1.5nM，2nM，2nM，5nM，6nM，6nM，8nM，0.5nM，29nM，5nM，和9nM[1]。Sitravatinib单独使⽤即具有有效的抗肿瘤功效，且通过促进抗肿瘤免疫微环境增强了PD-1阻断的活性[2]。IC50&TargetVEGFR3VEGFR1VEGFR2TrkA2nM(IC50)6nM(IC50)5nM(IC50)5nM(IC50)TrkBDDR1DDR2Axl9nM(IC50)29nM(IC50)0.5nM(IC50)1.5nM(IC50)MERFLT3KIT2nM(IC50)8nM(IC50)6nM(IC50)体外研究Sitravatinib(0.01nM-10μM;14days)reducescolonyformationinadose-dependentmannerinKLN205andE0771celllines[2].Sitravatinib(0.001-10μM;5days)inhibitstumorcellviabilitywithIC50sofapproximately1μMinKLN205,E0771andCT1B-A5celllines[2].CellViabilityAssay[2]CellLine:KLN205,E0771,CT1B-A5cellsConcentration:0.001,0.01,0.1,1,10μMIncubationTime:5daysResult:InhibitedKLN205,E0771,CT1B-A5cellswithIC50sofapproximately1μM.体内研究Sitravatinib(20mg/kg;p.o.;onceperdayfor6days)significantlyinhibitstumorprogressionandinducestumorregressioninC57BL/6micebearingCT1B-A5cellsmodel[2].2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:6-week-oldC57BL/6mice(bearingCT1B-A5cells)[2]Dosage:20mg/kgAdministration:Oraladministration;onceperdayfor6daysResult:Significantlyinhibitedtumorprogressionandinducedtumorregression.REFERENCES[1].PatwardhanPPetal.SignificantblockadeofmultiplereceptortyrosinekinasesbyMGCD516(Sitravatinib),anovelsmallmoleculeinhibitor,showspotentanti-tumoractivityinpreclinicalmodelsofsarcoma.Oncotarget,2016Jan26;7(4):4093-109.[2].DuW,etal.Sitravatinibpotentiatesimmunecheckpointblockadeinrefractorycancermodels.JCIInsight.2018Nov2;3(21).pii:124184.McePdfHeightCaution:Producthasnotbeenfully