BI-1347-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBI-1347Cat.No.:HY-120350CASNo.:2163056-91-3分?式:C??H??N?O分?量:356.42作?靶點:CDK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:125mg/mL(350.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8057mL14.0284mL28.0568mL5mM0.5611mL2.8057mL5.6114mL10mM0.2806mL1.4028mL2.8057mL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(fù)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(dāng)?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(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(5.84mM);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:≥2.08mg/mL(5.84mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.84mM);ClearsolutionBIOLOGICALACTIVITY?物活性BI-1347?種具有?服活性的、選擇性和強效的CDK8抑制劑(IC50=1.1nM)，且具有抗腫瘤活性。IC50&TargetCDK81.1nM(IC50)體外研究BI-1347(150nM;44h)enhancesgranzymeB(GZMB+)productioninmousesplenicNKcells[2].BI-1347(0.1nM-10μM;24h)treatmentincreasesperforinsecretionfromNK92MIcells[2].WesternBlotAnalysis[2]CellLine:MousesplenicNKcellsConcentration:150nMIncubationTime:44hoursResult:IncreasedtheproportionofgranzymeB-positiveNKcellsbyapproximately4-fold.WesternBlotAnalysis[2]CellLine:HumanNK92MIcellsConcentration:0.1nM-10μMIncubationTime:24hoursResult:IncreasedperforinlevelswithanEC50valueof7.2nM.體內(nèi)研究BI-1347(oralgavage;10mg/kg;oncedaily;30d)modulatesSTAT1S727phosphorylationandshowsanti-tumoractivityinvivo[2].BI-1347(oralgavage;10mg/kg)intermittentscheduleandBI-8382continuoustreatmentcombinationtreatmentincreasesefficacycomparedtoeachmonotherapyinthemammarycarcinomaEMT6model[2].AnimalModel:B16-F10-luc2syngeneicmelanomamodel[2]Dosage:10mg/kgAdministration:Oralgavage;10mg/kg;oncedaily;30d2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:ReducedphosphorylationofSTAT1S727foratleast6hby60%.Showedminimaleffectonbodyweightat10mg/kg.Showedlowertumorburdenbothonday23and29,comparedtothecontrolgroup.戶使?本產(chǎn)品發(fā)表的科研?獻?Cell.2021Apr15;184(8):2167-2182.e22.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HofmannMH,etal.SelectiveandPotentCDK8/19InhibitorsEnhanceNK-CellActivityandPromoteTumorSurveillance.MolCancerTher.2020Apr;19(4):1018-1030.[2].HaraldEngelhardt,etal.Newphenylpyrazolylacetamidecompoundsandderivativesascdk8/cdk19inhibitors.McePdfHeightCaution:Producthasnotbeenfullyvalidatedforme