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

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERineterkibCat.No.:HY-114491CASNo.:1715025-32-3分?式:C??H??BrF?N?O?分?量:578.42作?靶點:ERK;Raf作?通路:MAPK/ERKPathway;StemCell/Wnt儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:200mg/mL(345.77mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7288mL8.6442mL17.2885mL5mM0.3458mL1.7288mL3.4577mL10mM0.1729mL0.8644mL1.7288mL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(sealedstorage,awayfrommoistureandlight)。-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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(8.64mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Rineterkib(compoundB)具有?服活性的ERK1和ERK2的抑制劑，通過激活MAPK通路中的突變來發(fā)揮抗增?作?。這種活性與KRAS-突變型??細(xì)胞肺癌、BRAF-突變型??細(xì)胞肺癌、KRAS-突變型胰腺癌、KRAS-突變型結(jié)腸癌以及KRAS突變型巢癌尤為相關(guān)。Rineterkibhydrochloride也能抑制RAF。IC50&TargetERK1ERK2RAF體內(nèi)研究Rineterkib(compoundB)(50,75mg/kg,p.o.,qd/q2d,27days)treatmentsignificantlyreducesthetumorvolumeintheCalu-6humanNSCLCsubcutaneoustumorxenograftmodelinmice[1].AnimalModel:Calu-6NSCLCxenografttumormodelsinmice[1].Dosage:50,75mg/kg.Administration:Orallyeitherdaily(qd)oreveryotherday(q2d)for27days.Result:Significantlyreducedthetumorvolume.REFERENCES[1].SongY,etal.TargetingRAS-RAF-MEK-ERKsignalingpathwayinhumancancer:currentstatusinclinicaltrials.Genes&Diseases,2022.[2].CAPONIGRO,etal.THERAPEUTICCOMBINATIONSCOMPRISINGARAFINHIBITORANDAERKINHIBITOR.WO2018051306A1.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4