BAY-8002-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBAY-8002Cat.No.:HY-122312CASNo.:724440-27-1分?式:C??H??ClNO?S分?量:415.85作?靶點(diǎn):MonocarboxylateTransporter作?通路:MembraneTransporter/IonChannel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:125mg/mL(300.59mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.4047mL12.0236mL24.0471mL5mM0.4809mL2.4047mL4.8094mL10mM0.2405mL1.2024mL2.4047mL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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(5.00mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.00mM);Suspendedsolution;Needultrasonic3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性BAY-8002?種有效、選擇性、可?服的單羧酸轉(zhuǎn)運(yùn)蛋?第1亞型(monocarboxylatetransporter1(MCT1))抑制劑，在表達(dá)MCT1的DLD-1細(xì)胞中，IC50值為85nM，對(duì)MCT1的選擇性遠(yuǎn)?于MCT4。具有抗腫瘤活性[1]。IC50&TargetIC50:85nM(MCT1,inDLD-1cells)[1]體外研究BAY-8002isaninhibitorofMCT1,withanIC50of85nMintheMCT1-expressingDLD-1cells,displaysexcellentselectivityagainstMCT4(IC50>50μMinEVSA-Tcells)[1].體內(nèi)研究BAY-8002(80and160mg/kg,p.o.,twicedaily,formorethan26days)significantlyinhibitstumorgrowthinRajitumor-bearingmice[1].AnimalModel:FemaleNODSCIDmicebearingRajicells(7-10weeksold)[1]Dosage:80and160mg/kgAdministration:P.O.twicedailyformorethan26daysResult:Inhibitedtumorgrowthwithnoobviousbodyweightloss,butshowednoeffectontumorregression.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Cell.2021Jan21;184(2):370-383.e13.?Blood.2021Oct5;blood.2021011563.?CritRevAnalChem.2021Mar10;1-15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].QuanzM,etal.PreclinicalEfficacyoftheNovelMonocarboxylateTransporter1InhibitorBAY-8002andAssociatedMarkersofResistance.MolCancerTher.2018Nov;17(11):2285-2296.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forrese