PACMA-31-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPACMA31Cat.No.:HY-100433CASNo.:1401089-31-3分?式:C??H??N?O?S分?量:430.47作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(232.30mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3230mL11.6152mL23.2304mL5mM0.4646mL2.3230mL4.6461mL10mM0.2323mL1.1615mL2.3230mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。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。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(5.81mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.81mM);ClearsolutionBIOLOGICALACTIVITY?物活性PACMA31?種不可逆的?服活性蛋??硫化物異構酶(PDI)抑制劑，IC50為10μM，PACMA31與PDI的活性部位半胱氨酸形成共價鍵。PACMA31具有腫瘤靶向性，能顯著抑制巢腫瘤?長，對正常組織?毒性。IC50&TargetIC50:10μM(proteindisulfideisomerase)[1]體外研究PACMA31(0-10μM;24hours)significantlyinhibitscolonyformationinOVCAR-8cellsinadose-dependentmanner[1].體內研究PACMA31(20-200mg/kg;i.p.;dailyfor62days)suppressestumorgrowthinhumanovariancancermousexenografts[1].AnimalModel:Athymicmice(bearingOVCAR-8cells)[1]Dosage:20-200mg/kgAdministration:I.p.,perdayforthefirst3wkwith5-donand2-dofftreatmentcycles,anddosewasescalatedto40mg/kgperdayforthenext7d;p.o.,theinitialdoseof20mg/kgperdaywasgraduallyincreasedby20mg/kgperdaywitheachdosefor3dbeforeitwasorallydosedat200mg/kgperdayforanadditional32d,increasingthedosefrom20to200mg/kgResult:Comparedwiththecontrolgroup,i.p.orperosadministrationofPACMA31significantlyinhibitedtumorgrowthby85%and65%atday62,respectively.REFERENCES[1].XuS,etal.Discoveryofanorallyactivesmall-moleculeirreversibleinhibitorofproteindisulfideisomeraseforovariancancertreatment.ProcNatlAcadSciUSA.2012;109(40):16348-16353.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch