OBI-3424-TH-3424-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEOBI-3424Cat.No.:HY-124573CASNo.:2097713-68-1Synonyms:TH-3424分⼦式:C₂₁H₂₅N₄O₆P分⼦量:460.42作⽤靶点:DNAAlkylator/Crosslinker作⽤通路:CellCycle/DNADamage储存⽅式:-20°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:50mg/mL(108.60mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1719mL10.8596mL21.7193mL5mM0.4344mL2.1719mL4.3439mL10mM0.2172mL1.0860mL2.1719mL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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。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。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(10.86mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.43mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性OBI-3424(TH-3424)⼀种前药，可通过AKR1C3(醛酮还原酶1C3)选择性地转化为有效的DNA烷化剂。OBI-3424可⽤于肝细胞癌，去势抵抗性前列腺癌和急性淋巴细胞⽩⾎病(ALL)的研究。体外研究OBI-3424exertspotentcytotoxicityagainsttheH460lungcancercellline(IC50of4.0nM).OBI-3424exhibitspotentcytotoxicity,inparticularagainstcelllinesderivedfromT-ALLwithhighAKR1C3expression,withIC50valuesinthelownMrange[1].OBI-3424alsoexertspotentcellkillingagainstALLPDXs,andthemedianIC50valueswere60.3nMforB-ALL,9.7nMforT-ALLand31.5nMforETP-ALL[1].体内研究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