LG100268-LG268-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemELG100268Cat.No.:HY-15340CASNo.:153559-76-3Synonyms:LG268分⼦式:C₂₄H₂₉NO₂分⼦量:363.49作⽤靶点:RAR/RXR;Autophagy作⽤通路:MetabolicEnzyme/Protease;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:4.17mg/mL(11.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.7511mL13.7555mL27.5111mL5mM0.5502mL2.7511mL5.5022mL10mM0.2751mL1.3756mL2.7511mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(3.44mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(3.44mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoil1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.25mg/mL(3.44mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性LG100268(LG268)⼀种有效的、选择性的，具有⼝服活性的视素X受体(RXR)激动剂，对RXR-α，RXR-β，和RXR-γ的EC50值分别为4nM、3nM、4nM。LG100268显⽰对RXR的选择性优于RAR(1000倍)，对RXR-α，RXR-β，和RXR-γ的Ki值分别为3.4nM，6.2nM和9.2nM。LG100268激活RXR同⼆聚体，诱导转录激活。LG100268可⽤于肺癌的研究。体外研究LG100268(100nM-1μM;24hours)showsadownregulationofCSF3anda2.5-folddecreaseofCXCL2andIL-1βmRNAexpressioninRAW264.7cells[3].CellViabilityAssay[3]CellLine:RAW264.7cellsConcentration:100nM-1μMIncubationTime:24hoursResult:DecreasedLPSinducedcytokinemRNAlevels.体内研究LG100268(oraldiet;100mg/kg;oncedaily;7weeks)combineswithC/PpresentsamoremarkedlyreducedaveragetumorburdenthanLG268orC/Palone.Thecombinationestablishareducedlungtumors,whichrepresentsareductionof82%(vs.59%-67%withthesingledrugs)incomparisonwiththecontrols[3].AnimalModel:A/Jmice[3]Dosage:50mg/kg(Combineswithcarboplatin(50mg/kgi.p.)starts1weekaftertheLG268treatmentdiet)Administration:Oraldiet;oncedaily;7weeksResult:Decreasedlungtumorsgrowthsignificantlyinmice.REFERENCES[1].MFBoehm,etal.DesignandSynthesisofPotentRetinoidXReceptorSelectiveLigandsThatInduceApoptosisinLeukemiaCells.JMedChem[2].DSLala,etal.ActivationofSpecificRXRHeterodimersbyanAntagonistofRXRHomodimers.Nature.1996Oct3;383(6599):450-3.[3].MartineCao,etal.TheRexinoidsLG100268andLG101506InhibitInflammationandSuppressLungCarcinogenesisinA/JMice.CancerPrevRes(Phila).2016Jan;9(1):105-14.McePdfHeight2/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalappl