HDACs-mTOR-Inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEHDACs/mTORInhibitor1Cat.No.:HY-114414CASNo.:2271413-06-8分⼦式:C₂₈H₃₈N₈O₅分⼦量:566.65作⽤靶点:HDAC;mTOR;Apoptosis作⽤通路:CellCycle/DNADamage;Epigenetics;PI3K/Akt/mTOR;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:32.5mg/mL(57.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7648mL8.8238mL17.6476mL5mM0.3530mL1.7648mL3.5295mL10mM0.1765mL0.8824mL1.7648mL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。-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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.17mg/mL(3.83mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.83mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性HDACs/mTORInhibitor1⼀种双重的HDACs和mTOR抑制剂，对HDAC1,HDAC6,mTOR的IC50s分别为0.19nM、1.8nM、1.2nM。HDACs/mTORInhibitor1刺激细胞周期停滞在G0/G1期并诱导肿瘤细胞凋亡，且invivo毒性低。HDACs/mTORInhibitor1可⽤于⾎液系统恶性肿瘤的研究。IC50&TargetHDAC1HDAC6mTOR0.19nM(IC50)1.8nM(IC50)1.2nM(IC50)体外研究HDACs/mTORInhibitor1(Compound12l)inhibitsleukemiacellsproliferationwithIC50sof4.05,9.01,9.98μMforMV4-11,OCI-AML2,OCI-AML3cells[1].HDACs/mTORInhibitor1(0-10μM,6hor24h)downregulatesp-ERKandincreasesAc-H3inMV4-11cells[1].HDACs/mTORInhibitor1(10to1000nM,48h)reducesS-phasecellsandincreasesthepercentageofcellsinG0/G1phaseinMV4-11cells[1].WesternBlotAnalysis[1]CellLine:MV4-11cellsConcentration:0.01,0.1,1,10μMIncubationTime:6hor24hResult:Downregulatedp-ERK(24h)andincreasedoftheAc-H3(6h)inadose-dependentmanner.体内研究HDACs/mTORInhibitor1(Compound12l)(10or20mg/kg,i.v.)inhibitstumorgrowthwithoutsignificanttoxicityinMV4-11andMM1SxenograftNOD/SCIDmousemodel[1].AnimalModel:MV4-11xenograftNOD/SCIDmousemodel[1]Dosage:10mg/kgAdministration:Intravenousinjection(i.v.),everytwodays(Q2D)×6Result:TheTGI(tumorgrowthinhibitoryrate)was53.1%.户使⽤本产品发表的科研⽂献2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•FrontPharmacol.2020Nov11;11:580407.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChenY,etal.DiscoveryofaNovelDualHistoneDeacetylases(HDACs)andMammalianTargetofRapamycin(mTOR)TargetInhibitorasaPromisingStrategyforCancerTherapy.JMedChem.2019Jan10.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap