OTX008-Calixarene-0118-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEOTX008Cat.No.:HY-19756CASNo.:286936-40-1Synonyms:Calixarene0118;PTX008分?式:C??H??N?O?分?量:937.18作?靶點:Galectin作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗Ethanol:12.5mg/mL(13.34mM;Needultrasonic)DMSO:6.25mg/mL(6.67mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.0670mL5.3352mL10.6703mL5mM0.2134mL1.0670mL2.1341mL10mM0.1067mL0.5335mL1.0670mL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(fù)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(dāng)?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(dāng)保存；體內(nèi)實驗的?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)1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(1.07mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(1.07mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(1.07mM);Clearsolution4.請依序添加每種溶劑：10%EtOH>>90%SalineSolubility:≥1.25mg/mL(1.33mM);Clearsolution5.請依序添加每種溶劑：PBSSolubility:0.5mg/mL(0.53mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性O(shè)TX008?個半乳糖凝集素1(galectin-1)的選擇性抑制劑。IC50&TargetGalectin-1[1].體外研究Growthinhibitoryconcentrations(GI50)ofOTX008inalargepanelofhumansolidtumourcelllinesrangesfrom3to500μM.AsignificantcorrelationbetweenOTX008GI50valuesandGal1mRNA(LGALS1)andproteinexpressionlevelsinthepanelofcancercellsisobserved.InSQ20BandA2780-1A9cells,OTX008inhibitsGal1expressionandERK1/2andAKT-dependentsurvivalpathways,andinducesG2/McellcyclearrestthroughCDK1.OTX008enhancestheanti-proliferativeeffectsofSemaphorin-3A(Sema3A)inSQ20BcellsandreversesinvasioninducedbyexogenousGal1[1].OTX008affectsendothelialcellproliferation,motility,invasiveness,andcordformation.Tumorcellproliferationisalsoinhibited,withdifferencesinsensitivityamongcelllines(IC50from1to190μM)[2].體內(nèi)研究OTX008inhibitsgrowthofA2780-1A9xenografts.OTX008treatmentisassociatedwithdown-regulationofGal1andKi67intreatedtumours,aswellasdecreasedmicrovesseldensityandVEGFR2expression.Finally,combinationstudiesshowOTX008synergywithseveralcytotoxicandtargetedtherapies,principallywhenOTX008isadministeredfirst[1].PROTOCOLAnimalMice[1]Administration[1]Atotalof8×106A2780-1A9ovariancellsareinjectedsubcutaneouslyintotherightlateralflankoffemalenu/nuathymicmice.Oncetumoursarepalpable(50mm3),micearerandomisedtoreceivetreatmentintraperitoneallywitheitherPBS(3times/week),5mg/kgOTX008(3times/week),6mg/kgcisplatin(days1,8and15)or10mg/kgdocetaxel(days1,8and15).Tumoursizewasmeasuredtwiceweeklywithcalipersandtumourvolumeiscalculatedas3.14×(width2)/length[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CellRep.2021Aug31;36(9):109647.?CancerLett.2020Jan28;469:287-300.?Cells.2021,10(5),1112.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Astorgues-XerriL,etal.OTX008,aselectivesmall-moleculeinhibitorofgalectin-1,downregulatescancercellproliferation,invasionandtumourangiogenesis.EurJCancer.2014Sep;50(14):2463-77.[2].ZucchettiM,etal.Pharmacokineticsandantineoplasticactivityofgalectin-1-targetingOTX008incombinationwithsunitinib.CancerChemotherPharmacol.2013Oct;72(4):879-87.McePdfHeightCau