Naquotinib-mesylate-ASP8273-mesylate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENaquotinibmesylateCat.No.:HY-19803CASNo.:1448237-05-5Synonyms:ASP8273(mesylate)分?式:C??H??N?O?S分?量:658.81作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:12.5mg/mL(18.97mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.5179mL7.5894mL15.1789mL5mM0.3036mL1.5179mL3.0358mL10mM0.1518mL0.7589mL1.5179mL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,awayfrommoisture)。-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:≥2mg/mL(3.04mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2mg/mL(3.04mM);ClearsolutionBIOLOGICALACTIVITY?物活性Naquotinibmesylate(ASP8273mesylate)有?服活性，不可逆的EGFR突變體抑制劑；對EGFR突變體和EGFR的IC50值分別為8-33和230nM。IC50&TargetEGFRL858R/T790MEGFRL858REGFRExon19EGFRExon19(IC50)(IC50)deletiondeletion/T790M(IC50)(IC50)EGFR230nM(IC50)體外研究InassaysusingendogenouslyEGFR-dependentcells,NaquotinibinhibitsthegrowthofPC-9(delex19),HCC827(delex19),NCI-H1975(delex19/T790M)andPC-9ER(delex19/T790M)withIC50sof8-33nM[1].NaquotinibselectivelyinhibitsphosphorylationofEGFRanditsdown-streamsignalpathway,ERKandAktfrom10nMinHCC827andNCI-H1975whileinhibitoryeffectsareonlydetectedat1000nMinA431.InNCI-H1650(delex19),NaquotinibinhibitscellgrowthwithanIC50valueof70nMwhileotherEGFR-TKIsareonlypartiallyeffective[2].體內(nèi)研究OralNaquotinibtreatmentdosedependentlyinducestumorregressioninNCI-H1975(L858R/T790M),HCC827(delex19)andPC-9(delex19)xenograftmodels.DosingschedulesdoesnotaffecttheefficacyofNaquotinib.InanNCI-H1975xenograftmodel,completeregressionoftumorisachievedafter14-daysofNaquotinibtreatment.Completeregressionismaintainedin50%ofmicemorethan85daysaftercessationofNaquotinibtreatment[2].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?RSCAdv.2019,9(18):10211-10225.?RSCAdv.2019,9,4862-4869?RSocOpenSci.2019Jun5;6(6):190434.?bioRxiv.2020Jun.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SakagamiH,etal.ASP8273,anovelmutant-selectiveirreversibleEGFRinhibitor,inhibitsgrowthofnon-smallcelllungcancer(NSCLC)cellswithEGFRactivatingandT790Mresistancemutations.[abstract].In:Proceedingsofthe105thAnnualMeetingoft[2].KonagaiS,etal.ASP8273selectivelyinhibitsmutantEGFRsignalpathwayandinducestumorshrinkageinEGFRmutatedtumormodels.[abstract].In:Proceedingsofthe106thAnnualMeetingoftheAmericanAssociationforCancerResearch;2015Apr18-22;Ph2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasnotbeenfully