ARN-3236-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEARN-3236Cat.No.:HY-120856CASNo.:1613710-01-2分?式:C??H??N?O?S分?量:336.41作?靶點:Salt-inducibleKinase(SIK)作?通路:Immunology/Inflammation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(297.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9726mL14.8628mL29.7256mL5mM0.5945mL2.9726mL5.9451mL10mM0.2973mL1.4863mL2.9726mL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:≥2.17mg/mL(6.45mM);Clearsolution1/3MasterofBioactiveMolecules—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:≥2.17mg/mL(6.45mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.17mg/mL(6.45mM);ClearsolutionBIOLOGICALACTIVITY?物活性ARN-3236具有?服活性的鹽誘導激酶2(SIK2)的選擇性抑制劑，其對SIK2、SIK1和SIK3的IC50值分別為[1][2]。IC50&TargetSIK2SIK1SIK350)21.63nM(IC50)6.63nM(IC50)體外研究ARN-3236inhibitsSIK2activitywithanIC50[2].ARN-3236inhibitscellgrowthandincreasesNSC125973sensitivityinovariancancercells[2].CellViabilityAssay[2]CellLine:HEYandA2780humanovariancancercelllines.Concentration:0-10μM.IncubationTime:24hours.Result:InhibitedSIK2activitywithanIC50<1nM.體內(nèi)研究ARN-3236(60mg/kg,orally)sensitizesovariancancertoNSC125973invivo[2].AnimalModel:SKOv3ip-bearingmiceandOVCAR8-bearingmice[2].Dosage:60mg/kg.Administration:Orallyoncedailyfor3weeks(SKOv3ip-bearingmice)and4weeks(OVCAR8-bearingmice).Result:SensitizedovariancancertoNSC125973.戶使?本產(chǎn)品發(fā)表的科研?獻?TranslRes.2022Sep5;S1931-5244(22)00198-0.?Oncogene.2022Mar11.?BMCPulmMed.2022Apr11;22(1):140.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].LombardiMS,etal.SIKinhibitioninhumanmyeloidcellsmodulatesTLRandIL-1Rsignalingandinducesananti-inflammatoryphenotype.JLeukocBiol.2016May;99(5):711-21.[2].ZhouJ,etal.ANovelCompoundARN-3236InhibitsSalt-InducibleKinase2andSensitizesOvarianCancerCellLinesandXenografts.ClinCancerRes.2017Apr15;23(8):1945-1954.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio