Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAlmonertinibhydrochlorideCat.No.:HY-112823BCASNo.:2134096-03-8Synonyms:HS-10296hydrochloride分?式:C??H??ClN?O?分?量:562.11作?靶點(diǎn):EGFR作?通路:JAK/STATSignaling;ProteinTyrosineKinase/RTK儲(chǔ)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(shí)驗(yàn)DMSO:83.33mg/mL(148.25mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7790mL8.8951mL17.7901mL5mM0.3558mL1.7790mL3.5580mL10mM0.1779mL0.8895mL1.7790mL請(qǐng)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(qǐng)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(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.70mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.70mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.70mM);ClearsolutionBIOLOGICALACTIVITY?物活性Almonertinib(HS-10296)hydrochloride?種?服、不可逆的第三代EGFR酪氨酸激酶抑制劑，對(duì)EGFR致敏和T790M耐藥突變具有?選擇性。Almonertinibhydrochloride對(duì)T790M、T790M/L858R和T790M/Del19表現(xiàn)出較強(qiáng)的抑制活性(IC50分別為0.37、0.29和0.21nM)，對(duì)野?型的抑制作?較弱(3.39nM)。Almonertinibhydrochloride?于??細(xì)胞肺癌的研究。IC50&TargetEGFRT790MEGFRL858R/T790MEGFRdel19T790M0.37nM(IC50)0.29mM(IC50)0.214nM(IC50)體外研究Almonertinib(HS-10296)isanorallyavailableinhibitoroftheepidermalgrowthfactorreceptor(EGFR)mutantformT790M,withpotentialantineoplasticactivity,whichcanbeusedtotreatNSCLC[2].Additionaly,Almonertinib(HS-10296)couldalsoinhibitotherEGFRsensitivemutations,includingG719X,del19,L858RandL861Q[3].戶(hù)使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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