Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESU6656Cat.No.:HY-B0789CASNo.:330161-87-0分?式:C??H??N?O?S分?量:371.45作?靶點:Src;FAK;Akt作?通路:ProteinTyrosineKinase/RTK;PI3K/Akt/mTOR儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:20mg/mL(53.84mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.6922mL13.4608mL26.9215mL5mM0.5384mL2.6922mL5.3843mL10mM0.2692mL1.3461mL2.6922mL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:≥2mg/mL(5.38mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性SU6656Src家族激酶抑制劑，抑制Src，Yes，Lyn，F(xiàn)yn的IC50分別為280，20，130，170nM。SU6656可抑制FAKY576/577、Y925、Y861位點的磷酸化。SU6656還能抑制p-AKT。體外研究SU6656decreasesphosphorylationofSrcfamilykinases(SFKs)inHNSCCcells[2].體內(nèi)研究SU6656(2-4mg/kg;i.p.;once)significantlydecreasesischemicpostconditioning(IPoCo)mediatedincreaseinfalldowntime[5].AnimalModel:Swissalbinomalemice[5]Dosage:2,4mg/kgAdministration:Intraperitonealinjection;onceResult:SignificantlydecreasedIPoComediatedincreaseinfalldowntime.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?CancerRes.2021Jan1;81(1):187-198.?Theranostics.2020Jul9;10(19):8573-8590.?JMedChem.2021Sep3.?BiochimBiophysActaMolBasisDis.2018Nov;1864(11):3824-3836.?JAgricFoodChem.2021Jul29.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BlakeRA,etal.SU6656,aselectivesrcfamilykinaseinhibitor,usedtoprobegrowthfactorsignaling.MolCellBiol.2000Dec;20(23):9018-27.[2].VeraciniL,etal.ElevatedSrcfamilykinaseactivitystabilizesE-cadherin-basedjunctionsandcollectivemovementofheadandnecksquamouscellcarcinomas.Oncotarget.2014Dec26.[3].WuML,etal.DivergentsignalingpathwayscooperativelyregulateTGFβinductionofcysteine-richprotein2invascularsmoothmusclecells.CellCommunSignal.2014Mar28;12:22.[4].OndrusováL,etal.InhibitionofmTORC1bySU6656,theselectiveSrckinaseinhibitor,isnotaccompaniedbyactivationofAkt/PKBsignallinginmelanomacells.FoliaBiol(Praha).2013;59(4):162-7.[5].KumarA,etal.PharmacologicalinvestigationsonpossibleroleofSrckinasesinneuroprotectivemechanismofischemicpostconditioninginmice.IntJNeurosci.2014Oct;124(10):777-86.[6].LiuXF,etal.AntitumoreffectsofimmunotoxinsareenhancedbyloweringHCKortreatmentwithSRCkinaseinhibitors.MolCancerTher.2014Jan;13(1):82-9.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedform