OTS186935-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEOTS186935hydrochlorideCat.No.:HY-122181B分⼦式:C₂₅H₂₆ClN₅O₂.₈/₅HCl分⼦量:522.31作⽤靶点:HistoneMethyltransferase作⽤通路:Epigenetics储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:25mg/mL(47.86mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9146mL9.5729mL19.1457mL5mM0.3829mL1.9146mL3.8291mL10mM0.1915mL0.9573mL1.9146mL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，并请注意储备液的保存⽅式和期限。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，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(3.98mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.98mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.98mM);Clearsolution1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性OTS186935hydrochloride⼀种有效的蛋⽩甲转移酶SUV39H2抑制剂，IC50值为6.49nM。OTS186935hydrochloride对⼩⿏异种移植模型的肿瘤⽣长有明显的抑制作⽤，且⽆明显毒性。OTS193320hydrochloride调节癌细胞中γ-H2AX的产⽣。IC50&TargetIC50:6.49nM(SUV39H2)[1]体外研究OTS186935hydrochlorideinhibitsA549cellgrowthwithanIC50of0.67μM[1].体内研究OTS186935hydrochloride(10mg/kgor25mg/kg;intravenously;oncedailyfor14days)exhibitsgrowthsuppressiveeffectsinhumancancercelllinederivedxenograftmodels[1].AnimalModel:FemaleNOD.CB17-Prkdcscid/Jmice(bearingMDA-MB-231cells)[1]Dosage:10mg/kgAdministration:Intravenously;oncedailyfor14daysResult:Tumorgrowthinhibitionof42.6%onday14.AnimalModel:FemaleBALB/cAJcl-nu/numice(bearingA549cells)[1]Dosage:25mg/kgAdministration:Intravenously;oncedailyfor14daysResult:Yieldedatumorgrowthinhibitionof60.8%withoutsignificantbodyweightlossortoxicity.REFERENCES[1].VougiouklakisT,etal.DevelopmentofnovelSUV39H2inhibitorsthatexhibitgrowthsuppressiveeffectsinmousexenograftmodelsandregulatethephosphorylationofH2AX.Oncotarget.2018Aug7;9(61):31820-31831.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu