JND3229-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJND3229Cat.No.:HY-119944CASNo.:2260886-64-2分⼦式:C₃₃H₄₁ClN₈O₂分⼦量:617.18作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:12.5mg/mL(20.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.6203mL8.1014mL16.2027mL5mM0.3241mL1.6203mL3.2405mL10mM0.1620mL0.8101mL1.6203mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(2.03mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(2.03mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.03mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JND3229⼀种可逆性的EGFRC797S抑制剂，对EGFRL858R/T790M/C797S、EGFRWT和EGFRL858R/T790M的IC50值分别为5.8、6.8和30.5nM。JND3229具有较好的抗增殖活性，能有效地抑制体内肿瘤的⽣长。JND3229可⽤于癌症，尤其⾮⼩细胞癌的研究。IC50&TargetIC50:5.8nM(EGFRL858R/T790M/C797S),6.8nM(EGFRWT),30.5nM(EGFRL858R/T790M)[1].体外研究JND3229potentlyinhibitstheproliferationofBaF3cells(harboringtheEGFRL858R/T790M/C797SandEGFR19D/T790M/C797Smutations),NCI-H1975NSCLCcells(withEGFRT790Mmutation)andA431cancercells(overexpressingEGFRWT)withIC50valuesof0.51,0.32,0.31and0.27µM,respectively[1].JND3229(0.1,0.3,1,3,10µM;2h)potentlyinhibitsthephosphorylationofEGFRL858R/T790M/C797SandEGFR19D/T790M/C797SinengineeringBaF3cells[1].WesternBlotAnalysis[1]CellLine:BaF3cells(overexpressingEGFRL858R/T790M/C797SorEGFR19D/T790M/C797S)Concentration:0.1,0.3,1,3,10µMIncubationTime:2hResult:SignificantlyinhibitedthephosphorylationofEGFRL858R/T790M/C797SandEGFR19D/T790M/C797Sinadose-dependentmanner.体内研究JND3229(10mg/kg;i.p.;twicedailyfor10days)exhibitsanobvioussuppressionoftumorgrowth,andshowstargetinhibitioninvivo[1].AnimalModel:BALB/cmice(bearingestablishedBaF3-EGFR19D/T790M/C797Smousexenografttumorsmodel)[1].Dosage:10mg/kgAdministration:Intraperitonealinjection;twicedailyfor10days.Result:CausedanobvioussuppressionoftumorgrowthwithaTumorGrowthInhibition(TGI)valueof42.2%.Showedwelltolerancewithoutobviousbodyweightlossorotherobvioustoxicsigninthetreatedanimals.SignificantlydecreasedthelevelofphosphorylatedEGFR(p-EGFR)tinthetumortissues.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].LuX,etal.DiscoveryofJND3229asaNewEGFRC797SMutantInhibitorwithInVivoMonodrugEfficacy.ACSMedChemLett.2018Oct8;9(11):1123-1127.McePdfHeightCaution:Producthasnotbeenfullyvalidat