Almonertinib-hydrochloride-HS-10296-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAlmonertinibhydrochlorideCat.No.:HY-112823BCASNo.:2134096-03-8Synonyms:HS-10296hydrochloride分⼦式:C₃₀H₃₆ClN₇O₂分⼦量:562.11作⽤靶点:EGFR作⽤通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:83.33mg/mL(148.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.7790mL8.8951mL17.7901mL5mM0.3558mL1.7790mL3.5580mL10mM0.1779mL0.8895mL1.7790mL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(sealedstorage,awayfrommoisture)。-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:≥2.08mg/mL(3.70mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.70mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.70mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Almonertinib(HS-10296)hydrochloride⼀种⼝服、不可逆的第三代EGFR酪氨酸激酶抑制剂，对EGFR致敏和T790M耐药突变具有⾼选择性。Almonertinibhydrochloride对T790M、T790M/L858R和T790M/Del19表现出较强的抑制活性(IC50分别为0.37、0.29和0.21nM)，对野⽣型的抑制作⽤较弱(3.39nM)。Almonertinibhydrochloride⽤于⾮⼩细胞肺癌的研究。IC50&TargetEGFRT790MEGFRL858R/T790MEGFRdel19T790M0.37nM(IC50)0.29mM(IC50)0.214nM(IC50)体外研究Almonertinib(HS-10296)isanorallyavailableinhibitoroftheepidermalgrowthfactorreceptor(EGFR)mutantformT790M,withpotentialantineoplasticactivity,whichcanbeusedtotreatNSCLC[2].Additionaly,Almonertinib(HS-10296)couldalsoinhibitotherEGFRsensitivemutations,includingG719X,del19,L858RandL861Q[3].户使⽤本产品发表的科研⽂献•FrontPharmacol.2021May14;12:671328.•Patent.US20220177473A1.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].SullivanI,etal.Next-GenerationEGFRTyrosineKinaseInhibitorsforTreatingEGFR-MutantLungCancerbeyondFirstLine.FrontMed(Lausanne).2017Jan18;3:76.[2].WuSG,etal.ManagementofacquiredresistancetoEGFRTKI-targetedtherapyinadvancednon-smallcelllungcancer.MolCancer.2018Feb19;17(1):38.[3].YangJC,etal.Safety,Efficacy,andPharmacokineticsofAlmonertinib(HS-10296)inPretreatedPatientsWithEGFR-MutatedAdvancedNSCLC:AMulticenter,Open-label,Phase1Trial[publishedonlineaheadofprint,2020Sep9].JThoracOncol.2020;S1556-0McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalap