Vorasidenib-AG-881-DataSheet-生命科学试剂-MedChemExpressVIP

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEVorasidenibCat.No.:HY-104042CASNo.:1644545-52-7Synonyms:AG-881分⼦式:C₁₄H₁₃ClF₆N₆分⼦量:414.74作⽤靶点:IsocitrateDehydrogenase(IDH)作⽤通路:MetabolicEnzyme/Protease储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(241.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4111mL12.0557mL24.1115mL5mM0.4822mL2.4111mL4.8223mL10mM0.2411mL1.2056mL2.4111mL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。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:2.08mg/mL(5.02mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.02mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:2.08mg/mL(5.02mM);Clearsolution;Needwarming4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.5mg/mL(6.03mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:2.4mg/mL(5.79mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Vorasidenib(AG-881)⼀种可⼝服的、脑渗透的第⼆代突变体异柠檬酸脱氢酶1和2(mIDH1/2)双重抑制剂。Vorasidenib(AG-881)以纳尔抑制D-2-HG，对IDH1R132C、IDH1R132G、IDH1R132H、IDH1R132S的IC50值为0.04~22nM，对IDH2R140Q值为7~14nM，对IDH2R172K的值为130nM[1][2]。IC50&TargetIC50:0.04~22nM(IDH1R132C,IDH1R132G,IDH1R132H,IDH1R132S),7~14nM(IDH2R140Q),130nM(IDH2R172K)[2]体外研究VorasidenibhasstrongantiproliferativeactivityagainsthumanglioblastomaU-87MGpLVX-IDH2R140Q-neo,fibrosarcomaHT-1080andneurosphereTS603cells,allwithIC50soflessthan50nM[2].户使⽤本产品发表的科研⽂献•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