Erastin-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEErastinCat.No.:HY-15763CASNo.:571203-78-6分?式:C??H??ClN?O?分?量:547.04作?靶點:Ferroptosis;VDAC作?通路:Apoptosis;MembraneTransporter/IonChannel儲存?式:Powder-20°C3years4°C2years*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(22.85mM;Needultrasonic)掃描?維碼，H2O:<0.1mg/mL(insoluble)運?溶解?案計算器獲得適合您實驗體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.8280mL9.1401mL18.2802mL5mM0.3656mL1.8280mL3.6560mL10mM0.1828mL0.9140mL1.8280mL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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)?現(xiàn)配，即刻使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%DMSO40%PEG3005%Tween-8045%salineSolubility:2.08mg/mL(3.80mM);Suspendedsolution;Needultrasonic此?案可獲得2.08mg/mL(3.80mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。1/3www.MedChemEwww.MedChemE以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到400μLPEG300中，混合均勻；向上述2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請依序添加每種溶劑：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(3.80mM);Suspendedsolution;Needultrasonic此?案可獲得2.08mg/mL(3.80mM)的均勻懸濁液，懸濁液可?于?服和腹腔注射。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲備液加到900μL20%的SBE-β-CD?理鹽??溶3.液中，混合均勻。請依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥1.25mg/mL(2.29mM);Clearsolution此?案可獲得≥1.25mg/mL(2.29mM，飽和度未知)的澄溶液，此?案不適?于實驗周期在半個?以上的實驗。以1mL?作液為例，取100μL12.5mg/mL的澄DMSO儲備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Erastin鐵誘導的細胞死亡(ferroptosis)誘導劑。Erastin結(jié)合且抑制電壓依賴性離?通道(VDAC2/VDAC3)。體外研究Erastintriggersoxidative,iron-dependentcelldeath.TreatmentofNRAS-mutantHT-1080fibrosarcomacellswiththeRSLmoleculeerastin(10μM)resultsinatime-dependentincreaseincytosolicandlipidROSbeginningat2hours[1].Celldeathtriggeredbyerastinissignificantlyinhibitedbyantioxidants(e.g.,α-tocopherol,butylatedhydroxytoluene,andβ-carotene)andironchelators,suggestingthatROS-andiron-dependentsignalingisrequiredforerastin-inducedferroptosis.ErastincandirectlybindtoVDAC2/3inBJeLRcells.KnockdownofVDAC2andVDAC3,butnotVDAC1,leadstoerastinresistance.Erastinhastheabilitytoreduceglutathionelevelbydirectlyinhibitingcystine/glutamateantiportersystemXc?activity,withactivationoftheERstressresponse[2].ErastinpotentlyinhibitsHT-29cellsurvival.Erastinshowsadose-dependenteffect,and30μMoferastindisplaysthemostdramaticeffect[3].體內(nèi)研究Intraperitonealinjectionoferastinatwell-tolerateddosesdramaticallyinhibitsHT-29xenograftgrowthinseverecombinedimmunodeficientmice[3].PROTOCOLCellAssay[3]Totesterastin’sactivityoncolorectalcancercellsurvival,HT-29cellsaretreatedwithincreasingconcentrationsoferastin(0.1–30μM).MTTassaywasperformed[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice:Micearetreateddailywith10or30mg/kgbodyweightoferastin(intraperitonealinjection,for4weeks)Administration[3]orvehiclecontrol(Saline).Tumorvolumesarecalculated.Micebodyweightsarealsorecordedeveryweek[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻2/3www.MedChemEwww.MedChemE?CellDeathDiffer.2020Sep;27(9):2635-2650.?CellDeathDiffer.2021Apr;28(4):1222-1236.?CancerLett.2021Apr16;S0304-3835(21)00167-1.?CancerLett.2021Mar16;S0304-3835(21)00118-X.?JAdvRes.2020Jul22;28:231-243.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].DixonSJ,etal.Ferroptosis:aniron-dependentformofnonapoptoticcelldeath.Cell.2012May25;149(5):1060-72.[2].XieY,etal.Ferroptosis:processandfunction.CellDeathDiffer.2016Mar;23(3):369-79.[3].HuoH,etal.ErastinDisruptsMitochondrialPermeabilityTransitionPore(mPTP)andInducesApoptoticDeathofColorectalCancerCells.PLoSOne.2016May12;11(5):e0154605.McePdfHeight關(guān)注MCE中國公眾號，

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