HDACs-mTOR-Inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHDACs/mTORInhibitor1Cat.No.:HY-114414CASNo.:2271413-06-8分?式:C??H??N?O?分?量:566.65作?靶點(diǎn):HDAC;mTOR;Apoptosis作?通路:CellCycle/DNADamage;Epigenetics;PI3K/Akt/mTOR;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:32.5mg/mL(57.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7648mL8.8238mL17.6476mL5mM0.3530mL1.7648mL3.5295mL10mM0.1765mL0.8824mL1.7648mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)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(chǔ)備液可以根據(jù)儲(chǔ)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.17mg/mL(3.83mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(3.83mM);ClearsolutionBIOLOGICALACTIVITY?物活性HDACs/mTORInhibitor1?種雙重的HDACs和mTOR抑制劑，對(duì)HDAC1,HDAC6,mTOR的IC50s分別為0.19nM、1.8nM、1.2nM。HDACs/mTORInhibitor1刺激細(xì)胞周期停滯在G0/G1期并誘導(dǎo)腫瘤細(xì)胞凋亡，且invivo毒性低。HDACs/mTORInhibitor1可?于?液系統(tǒng)惡性腫瘤的研究。IC50&TargetHDAC1HDAC6mTOR0.19nM(IC50)1.8nM(IC50)1.2nM(IC50)體外研究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.體內(nèi)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%.戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?FrontPharmacol.2020Nov11;11:580407.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChenY,etal.DiscoveryofaNovelDualHistoneDeacetylases(HDACs)andMammalianTargetofRapamycin(mTOR)TargetInhibitorasaPromisingStrategyforCancerTherapy.JMedChem.2019Jan10.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap