WZ8040-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEWZ8040Cat.No.:HY-12029CASNo.:1214265-57-2分?式:C??H??ClN?OS分?量:481.01作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK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:25mg/mL(51.97mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0790mL10.3948mL20.7896mL5mM0.4158mL2.0790mL4.1579mL10mM0.2079mL1.0395mL2.0790mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1mg/mL(2.08mM);Clearsolution1/2MasterofBioactiveMolecules—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:≥1mg/mL(2.08mM);ClearsolutionBIOLOGICALACTIVITY?物活性WZ8040不可逆的、突變的EGFRT790M的抑制劑，可以抑制EGFR磷酸化。WZ8040對突變型EGFR的活性野?型EGFR的100倍以上。IC50&TargetEGFRDelE746_A750EGFRDelEGFRL858REGFRL858R/T790M1nM(IC50,inHCC827E746_A75066nM(IC50,in9nM(IC50,inH1975cells)6nM(IC50,inPC9H3255cells)cells)cells)EGFRDelEGFRERBB2ampERBB2ampE746_A750/T790ME746_A750/METamp738nM(IC50,in915nM(IC50,in8nM(IC50,inPC9GR>3.3μM(IC50,inH1819cells)Calu-3cells)cells)HCC827GRcells)ERBB2InsG776V,CEGFR&ERBB2WT744nM(IC50,inH17811.82μM(IC50,incells)HN11cells)體外研究WZ8040exhibitsIC50valuesof1nMforHCC827(EGFRDelE746_A750),6nMforPC9(EGFRDelE746_A750),66nMforH3255(EGFRL858R),9nMforH1975(EGFRL858R/T790M),8nMforPC9GR(EGFRDelE746_A750/T790M),>3.3μMforHCC827GR(EGFRE746_A750/METamp),738nMforH1819(ERBB2amp),915nMforCalu-3(ERBB2amp),744nMforH1781(ERBB2InsG776V,C),1.82μMforHN11(EGFR&ERBB2WT),respectively[1].WesternBlotAnalysis[1]CellLine:NSCLCcelllinesandBa/F3cells.Concentration:0-3.3μM.IncubationTime:24hours.Result:ExhibitedactivityforEGFR-mutatedNSCLClines,suchasHH827,PC9,H3255,H1819,Calu-3,H1781andHN11cells.REFERENCES[1].ZhouW,etal.Novelmutant-selectiveEGFRkinaseinhibitorsagainstEGFRT790M.Nature.2009Dec24;462(7276):1070-4.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplications.F