RPI-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemERPI-1Cat.No.:HY-101246CASNo.:269730-03-2分⼦式:C₁₇H₁₅NO₄分⼦量:297.31作⽤靶点:RET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:125mg/mL(420.44mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.3635mL16.8175mL33.6349mL5mM0.6727mL3.3635mL6.7270mL10mM0.3363mL1.6817mL3.3635mL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>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(7.00mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性RPI-1⼀种特异的⼝服2-吲哚啉酮Ret酪氨酸激酶抑制剂。RPI-1抑制⼈甲状腺髓样癌TT细胞增殖、Ret酪氨酸磷酸化、Ret蛋⽩表达及PLCgamma、ERKs和AKT的活化。具有抗肿瘤活性。体外研究TPC-1cellsaresensitivetothegrowthinhibitoryeffectofRPI-1withanIC50of5.1μM,following72hoursoftreatment.RPI-1(7.5-60µM)inhibitsRet/Ptc1autophosphorylationinTPC-1cells.RPI-1inhibitoryeffectsintheTPC-1cellcultureconditionsleadtoinhibitionofpathwaysinvolvingJNK2andAKT[1].TheRPI-1IC50valueforcellproliferationis3.6µMinNIH3T3cellsexpressingtheRetmutantcomparedwith16µMinnon-transfectedNIH3T3cells,andthatforcolonyformationinsoftagarwas2.4µMand26µMinRETmutant-transfectedandH-RAS-transfectedNIH3T3cells,respectively.InNIH3T3cellsexpressingtheRetmutant,Retproteinandtyrosinephosphorylationwereundetectableafter24hoursofRPI-1treatment.InTTcells,RPI-1inhibitsproliferation,Rettyrosinephosphorylation,Retproteinexpression,andtheactivationofPLCgamma,ERKsandAKT[2].体内研究RPI-1(50,100mg/kg;p.o.;twiceadayfor10days)inhibitsthetumorgrowthofTTxenograftsby81%[2].AnimalModel:8-to11-week-oldfemaleathymicnudeCD-1mice(bearingTTcells)[2]Dosage:50,100mg/kgAdministration:P.o.;twiceadayfor10daysResult:Adose-dependenteffectontumorgrowthwasobserved,withadoseof2*50mg/kg/dayresultinginlesstumorweightinhibitionthanthe2*100mg/kg/daydoseafter10daysoftreatment.REFERENCES[1].LanziC,etal.InactivationofRet/Ptc1oncoproteinandinhibitionofpapillarythyroidcarcinomacellproliferationbyindolinoneRPI-1.CellMolLifeSci.2003;60(7):1449-1459.[2].CuccuruG,etal.CellulareffectsandantitumoractivityofRETinhibitorRPI-1onMEN2A-associatedmedullarythyroidcarcinoma.JNatlCancerInst.2004;96(13):1006-1014.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical