IACS-010759-IACS-10759-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIACS-010759Cat.No.:HY-112037CASNo.:1570496-34-2Synonyms:IACS-10759分?式:C??H??F?N?O?S分?量:562.56作?靶點:MitochondrialMetabolism;Apoptosis作?通路:MetabolicEnzyme/Protease;Apoptosis儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:62.5mg/mL(111.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7776mL8.8879mL17.7759mL5mM0.3555mL1.7776mL3.5552mL10mM0.1778mL0.8888mL1.7776mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)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%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.08mg/mL(3.70mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性IACS-010759?種?服有效的線粒體氧化磷酸化復合物I(OXPHOS)抑制劑。IACS-010759在依賴OXPHOS的腦癌和急性髓性??病(AML)模型中抑制增殖并誘導細胞凋亡。IACS-010759具有?于復發(fā)/難治性AML和實體瘤研究的潛?。IC50&TargetOXPHOS[1]體外研究IACS-010759(10,30,100?nM;for4or5days)reducesviabilityandinducesapoptosisinprimaryAML[1].IACS-010759(0.001,0.01,0.1,1,10,100,1000nM;72hurs)robustlyinhibitsbothOCRandgalactose-dependentH460cellviabilityandhasnearlyidenticalIC50valuesof1.4?nM[1].IACS-010759issimilarlyactiveinmouse(averageIC50?=?5.6?nM),rat(IC50?=?12.2?nM),andcynomolgusmonkey(IC50?=?8.7?nM)celllines[1].IACS-010759(0.01-10μM)yieldesamaximalreductionofgrowthof?>?50%inthemajorityofcancercelllines(24of30pancreatic(PDAC),19of20ovarian,13of16triple-negativebreast(TNBC),8of10non-small-celllung(NSCLC))andasubset(11of30PDAC,10of20ovarian,5of16TNBC,2of10NSCLC)exhibited?>?100%growthinhibition[1].體內(nèi)研究IACS-010759(5,10,25?mg/kg/day;oral;for21d)resultsintumorregressionwithminimalbodyweightlossatthe5or10?mg/kgdoseinmicebearingNB-1(PGD-null)subcutaneousxenografts.IACS-010759atthe25?mg/kgdoseisnottolerated[1].IACS-010759HCl(10?mg/kg;orally;QD(daily)orQD×5(5don/2doff);for35d)increasesmediansurvivalfrom28dtolongerthan60d,whereasless-frequentdosingschedules(Q2DorQ3D)enhancessurvivaltoalesserextent[1].IACS-010759(0.3?mg/kgforiv;1?mg/kgfororal)haslowplasmaclearancewithahighvolumeofdistribution,resultinginaprolongedterminalhalf-life(>24?h)[1].戶使?本產(chǎn)品發(fā)表的科研?獻?CellDiscov.2022Oct6;8(1):102.?CellRepMed.2022Nov3;100802.?BiochemBiophysResCommun.2021Mar16;552:23-29.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ProtopopovaM.IACS-10759:AnovelOXPHOSinhibitorwhichselectivelykilltumorswithmetabolicvulnerabilities.[abstract].In:2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEProceedingsofthe106thAnnualMeetingoftheAmericanAssociationforCancerResearch;2015Apr18-22;Philadelphia,PA.Ph[2].JenniferRMolina,etal.Aninhibitorofoxidativephosphorylationexploitscancervulnerability.NatMed.2018Jul;24(7):1036-1046.McePdfHeightCaution:Producthasnotbee