MI-136-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMI-136Cat.No.:HY-19319CASNo.:1628316-74-4分?式:C??H??F?N?S分?量:470.51作?靶點:EpigeneticReaderDomain;AndrogenReceptor;Apoptosis作?通路:Epigenetics;Others;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:110mg/mL(233.79mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1254mL10.6268mL21.2535mL5mM0.4251mL2.1254mL4.2507mL10mM0.2125mL1.0627mL2.1254mL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(fù)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(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?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(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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:≥2.75mg/mL(5.84mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(5.84mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.75mg/mL(5.84mM);ClearsolutionBIOLOGICALACTIVITY?物活性MI-136menin-MLL(PPI)蛋?互作的抑制劑，其IC50值為31nM，Kd值為23.6nM。MI-136可抑制AR信號通路，有?于去勢抵抗性腫瘤的潛能。體外研究MI-136(0-20)exhibitsIC50valuesof5.59μM,7.15μM,5.37μMand19.76μMinLNCaP,VCaP,22rv1andPNT2cells[2].CellProliferationAssay[2]CellLine:ARpositivecelllinessuchasVCaP,LNCaPand22RV1.Concentration:0-20μM.IncubationTime:24h.Result:Inhibitedcellproliferation.體內(nèi)研究MI-136exhibitsT1/2of3.1hafterpoadministration[1].MI-136(40mg/kg,ip)leadstoasignificantdecreaseinthegrowthofcastration-resistantVCaPtumors[2].AnimalModel:VCaPxenografts[2].Dosage:40mg/kg.Administration:Intraperitonealinjection,5daysaweek.Result:Ledtoasignificantdecreaseinthegrowthofcastration-resistantVCaPtumorscomparedtovehiclecontrols.REFERENCES[1].DmitryBorkin,etal.PropertyFocusedStructure-BasedOptimizationofSmallMoleculeInhibitorsoftheProtein-ProteinInteractionbetweenMeninandMixedLineageLeukemia(MLL).JMedChem.2016Feb11;59(3):892-913.[2].RohitMalik,etal.TargetingtheMLLcomplexincastration-resistantprostatecancer.NatMed.2015Apr;21(4):344-52.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese