Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIDH1Inhibitor1Cat.No.:HY-112601CASNo.:2234285-81-3分?式:C??H??F?N?O?分?量:450.39作?靶點:IsocitrateDehydrogenase(IDH)作?通路:MetabolicEnzyme/Protease儲存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗DMSO:≥100mg/mL(222.03mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2203mL11.1015mL22.2030mL5mM0.4441mL2.2203mL4.4406mL10mM0.2220mL1.1101mL2.2203mL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(sealedstorage,awayfrommoistureandlight)。-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%salineSolubility:≥2.5mg/mL(5.55mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(5.55mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.55mM);ClearsolutionBIOLOGICALACTIVITY?物活性IDH1Inhibitor1?種有效的，?服?物可利?的，腦滲透性，選擇性突變IDH1抑制劑，抑制IDH1R132H，IDH1R132C，和IDH1WT，IC50分別為0.021μM,0.045μM,和2.52μM[1]。具有抗腫瘤活性[1]。IC50&TargetIC50:0.021μM(IDH1R132H),0.045μM(IDH1R132C),and2.52μM(IDH1WT)[1]體外研究IDH1Inhibitor1(Compound19)inhibitscellularHCT116-IDH1R132H/+withanIC50of0.039μM[1].體內(nèi)研究IDH1Inhibitor1(Compound19)inhibits2-hydroxyglutarate(2-HG)productioninapreclinicalxenografttumormodel.IDH1Inhibitor1isalsoprofiledinapatient-derivedIDH1mutantHCT116-IDH1R132H/+mechanisticxenografttumormodelinmicetoevaluateinvivoinhibitionof2-HGproduction.IDH1Inhibitor1,dosedorallyat150mg/kg,inhibitsnew2-HGproduction[1].REFERENCES[1].ZhaoQ,etal.Optimizationof3-Pyrimidin-4-yl-oxazolidin-2-onesasOrallyBioavailableandBrainPenetrantMutantIDH1Inhibitors.ACSMedChemLett.2018Jun11;9(7):746-751.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu