BAY885-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBAY885Cat.No.:HY-112082CASNo.:2307249-33-6分?式:C??H??F?N?O?分?量:515.53作?靶點(diǎn):ERK作?通路:MAPK/ERKPathway;StemCell/Wnt儲(chǔ)存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:16.67mg/mL(32.34mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9398mL9.6988mL19.3975mL5mM0.3880mL1.9398mL3.8795mL10mM0.1940mL0.9699mL1.9398mL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(storedundernitrogen)。-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：1%DMSO>>99%salineSolubility:0.5mg/mL(0.97mM);Suspendedsolution;Needultrasonic2.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.67mg/mL(3.24mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.67mg/mL(3.24mM);Clearsolution4.請(qǐng)依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(4.85mM);Clearsolution5.請(qǐng)依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(4.85mM);ClearsolutionBIOLOGICALACTIVITY?物活性BAY885?種?效的選擇性ERK5抑制劑，IC50為35nM，對(duì)其他激酶的抑制作?較弱。IC50&TargetERK535nM(IC50)體外研究TheERK5probe41(BAY-885)showedpotentERK5kinaseandtranscriptionalinhibitionintheSN12C-MEF2reportercellline(IC50=115nM/IC90=691nM)andhadnoeffectsonareportercontrolcelllinewithconstitutiveluciferaseexpression(SN12C-CMV-luc,IC50>30μM)[1].REFERENCES[1].NguyenD,etal.DiscoveryandCharacterizationofthePotentandHighlySelective(Piperidin-4-yl)pyrido[3,2-d]pyrimidineBasedinVitroProbeBAY-885fortheKinaseERK5.JMedChem.2019Jan24;62(2):928-940.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Te