Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEGusacitinibCat.No.:HY-103018CASNo.:1425381-60-7Synonyms:ASN-002分?式:C??H??N?O?分?量:460.53作?靶點(diǎn):JAK;Syk作?通路:Epigenetics;JAK/STATSignaling;ProteinTyrosineKinase/RTK;StemCell/Wnt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:100mg/mL(217.14mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.1714mL10.8571mL21.7141mL5mM0.4343mL2.1714mL4.3428mL10mM0.2171mL1.0857mL2.1714mL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)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.67mg/mL(3.63mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.67mg/mL(3.63mM);ClearsolutionBIOLOGICALACTIVITY?物活性Gusacitinib(ASN-002)?種有效的SYK激酶和JAK激酶的雙抑制劑，IC50值為5-46nM。Gusacitinib在實(shí)體和?液腫瘤中均具有抗癌活性。IC50&TargetIC50:5-46nM(SYK,JAK)[1].體外研究Inmechanisticcell-basedstudiesinvolvingIgEandcytokinestimulations,Gusacitinib(ASN-002)stronglysuppressestheSYKandJAKfamilykinasesignalingpathwaysmeasuredaspLATandpSTATlevels,respectively.Gusacitinib(ASN-002)showsanti-proliferativeactivityinabroadpanelofhumancancercelllinesincludingDHL6,DHL4,OCI-LY10,H929,Pfeiffer,HT-1376,andLovo,suggestingactivityinbothsolidandhematologicaltumortypes[1].體內(nèi)研究Inamultiplemyeloma(H929)xenograftmodel,Gusacitinib(ASN-002)exhibitssignificantefficacyininhibitingtumorgrowth(>95%).Italsosignificantlydelaystheonsetofhindlimbparalysisinthehumanerythroleukemia(HEL)mousemodel.Gusacitinib(ASN-002)hasgoodoralbioavailability,metabolicstability,isnotaPgpsubstrate,andshowslittletonoinhibitionofCYP450isozymes.Gusacitinib(ASN-002)showsafavorablesafetyprofileinratanddogtoxicologystudies[1].REFERENCES[1].SanjeevaReddy,etal.Abstract792:ASN002:AnoveldualSYK/JAKinhibitorwithstrongantitumoractivity.AACR106thAnnualMeeting2015;April18-22,2015;Philadelphia,PA.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forr