Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVorasidenibCat.No.:HY-104042CASNo.:1644545-52-7Synonyms:AG-881分?式:C??H??ClF?N?分?量:414.74作?靶點:IsocitrateDehydrogenase(IDH)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(241.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4111mL12.0557mL24.1115mL5mM0.4822mL2.4111mL4.8223mL10mM0.2411mL1.2056mL2.4111mL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備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:2.08mg/mL(5.02mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.02mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:2.08mg/mL(5.02mM);Clearsolution;Needwarming4.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.5mg/mL(6.03mM);Suspendedsolution;Needultrasonic5.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.4mg/mL(5.79mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Vorasidenib(AG-881)?種可?服的、腦滲透的第?代突變體異檸檬酸脫氫酶1和2(mIDH1/2)雙重抑制劑。Vorasidenib(AG-881)以納爾抑制D-2-HG，對IDH1R132C、IDH1R132G、IDH1R132H、IDH1R132S的IC50值為0.04~22nM，對IDH2R140Q值為7~14nM，對IDH2R172K的值為130nM[1][2]。IC50&TargetIC50:0.04~22nM(IDH1R132C,IDH1R132G,IDH1R132H,IDH1R132S),7~14nM(IDH2R140Q),130nM(IDH2R172K)[2]體外研究VorasidenibhasstrongantiproliferativeactivityagainsthumanglioblastomaU-87MGpLVX-IDH2R140Q-neo,fibrosarcomaHT-1080andneurosphereTS603cells,allwithIC50soflessthan50nM[2].戶使?本產(chǎn)品發(fā)表的科研?獻?Theranostics.2020Jul9;10(19):8757-8770.?Metabolites.2021Feb13;11(2):109.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FujiiT,etal.Targetingisocitratedehydrogenase(IDH)incancer.DiscovMed.2016May;21(117):373-80.[2].MaT,etal.InhibitorsofMutantIsocitrateDehydrogenases1and2(mIDH1/2):AnUpdateandPerspective.JMedChem.2018Oct25;61(20):8981-9003.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Fo