Terevalefim-ANG-3777-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETerevalefimCat.No.:HY-137455CASNo.:1070881-42-3Synonyms:ANG-3777分⼦式:C₉H₈N₂S分⼦量:176.24作⽤靶点:c-Met/HGFR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(567.41mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.6741mL28.3704mL56.7408mL5mM1.1348mL5.6741mL11.3482mL10mM0.5674mL2.8370mL5.6741mL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(14.19mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(14.19mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(14.19mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Terevalefim(ANG-3777)⼀种⼲细胞⽣长因⼦(HGF)的类似物，选择性的激活c-Met受体。体外研究Terevalefim(ANG-3777)(0-10μM)significantlyinhibitedcancercellsproliferationinHUVECs[2].CellViabilityAssay[2]CellLine:HumanUmbilicalVeinEpithelialCells(HUVECs).Concentration:0.44,1.78,and7.1μM.IncubationTime:24to48hours.Result:Dose-dependentlyinhibitedcellproliferation.体内研究Terevalefim(ANG-3777)decreasesapoptosis,increasesproliferation,andpromotesorganrepairandfunctioninanimalmodels[1].Terevalefim(ANG-3777,40mg/kg,IP)phosphorylatesthec-Metreceptorinrats[2].AnimalModel:SDrats[2].Dosage:40mg/kg.Administration:IPinjection,once.Result:Selectivelyphosphorylatedthec-Metreceptorandnotothergrowthfactorreceptors.REFERENCES[1].JonathanSBromberg,etal.RenalFunctionImprovementFollowingANG-3777TreatmentinPatientsatHighRiskforDelayedGraftFunctionAfterKidneyTransplantation.Transplantation.2021Feb1;105(2):443-450.[2].LathaPaka,etal.TheEffectofANG-3777onHepatocyteGrowthFactorReceptor,c-METSignaling.AmericanTransplantSociety.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc