CCG-1423-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECCG-1423Cat.No.:HY-13991CASNo.:285986-88-1分⼦式:C₁₈H₁₃ClF₆N₂O₃分⼦量:454.75作⽤靶点:Ras;Apoptosis作⽤通路:GPCR/GProtein;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:≥26mg/mL(57.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1990mL10.9951mL21.9901mL5mM0.4398mL2.1990mL4.3980mL10mM0.2199mL1.0995mL2.1990mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.50mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.50mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.50mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CCG-1423Rho/MRTF/SRF通路的抑制剂。CCG-1423在多种癌细胞中具有活性。CCG-1423开发新型药物⼯具的先导化合物，可⽤于癌症和糖尿病的研究。IC50&TargetIC50:1.5µM(Rho-pathwayselectiveserumresponseelement-luciferasereporter)[1]体外研究CCG-1423(10µM;24h)affectsinvasionbyculturedPC-3cellsintoaMatrigelmatrixandinhibits54%mitochondrialmetabolismofWST-1[1].CCG-1423(0-100µM;24h)inhibitsRhoAandRhoCsignalingpathwayswithanIC50valueof1.5µMforRho-pathwayselectiveserumresponseelement-luciferasereporter[1].CCG-1423(1µM;16h)improvesglucoseuptakeinbothL6cellsandprimaryhumanmyotubes[2].CCG-1423(10µM;18-19h)inhibitsexpressionofRhodownstream[2].CCG-1423(3µM;25h)selectivelystimulatesapoptosisofRhoC-overexpressingmelanomacellline(A375M2)comparedwiththeparentalcellline(A375)[3].CellInvasionAssay[1]CellLine:PC-3celllineConcentration:10µMIncubationTime:24hoursResult:Inhibited71%invasionbyculturedPC-3cellsintoaMatrigelmatrix.WesternBlotAnalysis[2]CellLine:L6myotubesConcentration:1µMIncubationTime:48hoursResult:Increasedinsulin-stimulatedAktphosphorylation,blockedERKphosphorylation,andincreasedIRS-1tyrosinephosphorylationanditsassociationwiththep85regulatorysubunitofPI3K.CellProliferationAssay[3]CellLine:PC-3cellline2/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEConcentration:0.3µMIncubationTime:8daysResult:InhibitedgrowthofPC-3prostatecancercellswithanIC50valueof1µMwith30µMLPAadding.ApoptosisAnalysis[3]CellLine:RhoC-overexpressingA375M2andlowRhoC-expressingA375melanomacelllinesConcentration:3µMIncubationTime:25hoursResult:StimulatedapoptosisofA375M2celllinecomparedwiththeparentalcellline.体内研究CCG-1423(0.15mg/kg;i.p.oncedailyfortwoweeks)affectsglucosetoleranceandinsulinlevelsinHFD-fedmice[1].AnimalModel:16-week-oldmicewithHFD-inducedobesity[1]Dosage:0.15mg/kgAdministration:Intraperitonealinjection;0.15mg/kgonceperday;fortwoweeksResult:Improvedglucosetoleranceandreducedinsulinlevelsat30minutesafterglucoseinjection.户使⽤本产品发表的科研⽂献•CellBiosci.2021Jan28;11(1):25.•ClinTranslMed.2022Jun;12(6):e850.•Cancers(Basel).2020Nov27;12(12):3540.•CommunBiol.2021Mar25;4(1):399.•Theriogenology.2019Oct15;138:84-93.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].EvelynCR,etal.CCG-1423:asmall-moleculeinhibitorofRhoAtranscriptionalsignaling.MolCancerTher.2007Aug;6(8):2249-60.[2].EvelynCR,etal.Design,synthesisandprostatecancercell-basedstudiesofanalogsoftheRho/MKL1transcriptionalpathwayinhibitor,CCG-1423.BioorgMedChemLett.2010Jan15;20(2):665-72.3/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[3].JinW,etal.IncreasedSRFtranscriptionalactivityinhumanandmouseskeletalmuscleisasignatureofinsulinresistance.JClinInvest.2011Mar;121(3):918-29.