Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemELQZ-7ICat.No.:HY-136538CASNo.:195822-23-2分?式:C??H??F?N?分?量:348.35作?靶點:Survivin作?通路:Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(358.83mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8707mL14.3534mL28.7068mL5mM0.5741mL2.8707mL5.7414mL10mM0.2871mL1.4353mL2.8707mL請根據(jù)產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；澄的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.97mM);ClearsolutionBIOLOGICALACTIVITY?物活性LQZ-7I?種靶向survivin的抑制劑。LQZ-7I抑制?存素?聚化。LQZ-7I?服有效抑制異種移植腫瘤?長并1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE誘導腫瘤中?存素的損失[1]。IC50&TargetSurvivin[1]體外研究LQZ-7IhasimprovedcytotoxicitywithIC50sof3.1μMagainstC4-2cellsand4.8μMagainstPC-3cellscomparedwiththeparentcompoundLQZ-7[1].LQZ-7I(10μM;0-6hours)treatmentreducestheexpressionofsurvivin.However,LQZ-7IdoesnotreducetheexpressionofXIAP,CIAP1,andCIAP2.LQZ-7Imaybeselectivetoitsintendedtargetsurvivin[1].WesternBlotAnalysis[1]CellLine:PC-3orC4-2cellsConcentration:10μMIncubationTime:0-6hoursResult:Reducedtheexpressionofsurvivin.體內研究LQZ-7I(100mg/kg;oralgavageeveryotherdayforatotaloftentreatments)significantlysuppressestumorgrowthwithoutanynotableadverseeffectonthemice[1].AnimalModel:6-weekoldmaleNSGmice[1]Dosage:100mg/kg;200μLvehicle(90%cornoil/10%DMSO)Administration:OralgavageeveryotherdayforatotaloftentreatmentsResult:Significantlysuppressedtumorgrowthwithoutanynotableadverseeffectonthemiceasindicatedbylackingchangesinbodyweightandinwetweightofmajororgansattheendofthestudy.REFERENCES[1].RobertPeery,etal.SynthesisandIdentificationofaNovelLeadTargetingSurvivinDimerizationforProteasome-DependentDegradation.JMedChem.2020Jun9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc