PD-407824-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPD407824Cat.No.:HY-18961CASNo.:622864-54-4分?式:C??H??N?O?分?量:328.32作?靶點:CheckpointKinase(Chk);Wee1作?通路:CellCycle/DNADamage儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(761.45mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.0458mL15.2290mL30.4581mL5mM0.6092mL3.0458mL6.0916mL10mM0.3046mL1.5229mL3.0458mL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%salineSolubility:≥2.08mg/mL(6.34mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.34mM);ClearsolutionBIOLOGICALACTIVITY?物活性PD407824?個檢查點激酶Chk1和WEE1抑制劑，IC50分別為47和97nM。PD407824?種化學BMP敏化劑，可提?細胞對亞閾值量的BMP4的敏感性。IC50&TargetChk1WEE147nM(IC50)97nM(IC50)體外研究PD407824issufficienttoblockCHK1,leadingtoasignificantdown-regulationofp21,causingactivationofCDK8/9,whichinturncausesdepletionofSMAD2/3[1].PD407824isselectiveforChk1andWEE1overPKCandCdk4withIC50sof3.4μMand3.75μM,respectively[3].REFERENCES[1].PalmerBD,etal.4-Phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dioneinhibitorsofthecheckpointkinaseWee1.Structure-activityrelationshipsforchromophoremodificationandphenylringsubstitution.JMedChem.2006Aug10;49(16):4896-911.[2].FengL,etal.DiscoveryofaSmall-MoleculeBMPSensitizerforHumanEmbryonicStemCellDifferentiation.CellRep.2016May31;15(9):2063-75.[3].SmaillJB,etal.Synthesisandstructure-activityrelationshipsofN-6substitutedanaloguesof9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-dionesasinhibitorsofWee1andChk1checkpointkinases.EurJMedChem.2008Jun;43(6):1276-96.Epub200McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse