Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOBI-3424Cat.No.:HY-124573CASNo.:2097713-68-1Synonyms:TH-3424分?式:C??H??N?O?P分?量:460.42作?靶點(diǎn):DNAAlkylator/Crosslinker作?通路:CellCycle/DNADamage儲存?式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1719mL10.8596mL21.7193mL5mM0.4344mL2.1719mL4.3439mL10mM0.2172mL1.0860mL2.1719mL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(protectfromlight)。-80°C儲存時，請?jiān)?個?內(nèi)使?，-20°C儲存時，請?jiān)?個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)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(shí)驗(yàn)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(shí)驗(yàn)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:≥5mg/mL(10.86mM);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:≥2.5mg/mL(5.43mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY?物活性O(shè)BI-3424(TH-3424)?種前藥，可通過AKR1C3(醛酮還原酶1C3)選擇性地轉(zhuǎn)化為有效的DNA烷化劑。OBI-3424可?于肝細(xì)胞癌，去勢抵抗性前列腺癌和急性淋巴細(xì)胞??病(ALL)的研究。體外研究OBI-3424exertspotentcytotoxicityagainsttheH460lungcancercellline(IC50of4.0nM).OBI-3424exhibitspotentcytotoxicity,inparticularagainstcelllinesderivedfromT-ALLwithhighAKR1C3expression,withIC50valuesinthelownMrange[1].OBI-3424alsoexertspotentcellkillingagainstALLPDXs,andthemedianIC50valueswere60.3nMforB-ALL,9.7nMforT-ALLand31.5nMforETP-ALL[1].體內(nèi)研究OBI-3424(0.5-2.5mg/kg;i.p.;onceweekly;for3weeks)treatmentinducesregressionsinPDXsmiceandresultsinprolongationofmouseevent-freesurvival[1].AnimalModel:FemaleNSGmice(20-25g)bearingpatient-derivedxenografts(PDX)[1]Dosage:0.5mg/kg,1mg/kg,2.5mg/kgAdministration:Intraperitonealinjection;onceweekly;for3weeksResult:Resultedinprolongationofmouseevent-freesurvival.REFERENCES[1].KathrynEvans,etal.OBI-3424,aNovelAKR1C3-ActivatedProdrug,ExhibitsPotentEfficacyagainstPreclinicalModelsofT-ALL.ClinCancerRes.2019Jul15;25(14):4493-4503.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese