CASIN-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECASINCat.No.:HY-12874CASNo.:425399-05-9分⼦式:C₂₀H₂₂N₂O分⼦量:306.4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:≥31mg/mL(101.17mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2637mL16.3185mL32.6371mL5mM0.6527mL3.2637mL6.5274mL10mM0.3264mL1.6319mL3.2637mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.79mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.79mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.79mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性CASIN⼀个选择性的GTPaseCdc42抑制剂，其IC50值2uM。CASIN可⽤于癌症的研究。IC50&TargetIC50:2μM(GTPaseCdc42)[1]体外研究CASIN(0-10μM;3d)inhibitsthegrowthofAMO-1,ARH-77,IM-9,JJN-3,L-363,MOLP-8andRPMI-8226/Scells[1].CASIN(0-10μM;16h)inhibitsmelphalaninducedFANCD2mono-ubiquitinationinLR5cellsbutshowsnoeffecttoScells[1].CASIN(5μM;2d)increasescellapoptosisofbortezomib-resistantMMpatientcells[1].CellViabilityAssay[3]CellLine:AMO-1,ARH-77,IM-9,JJN-3,L-363,MOLP-8andRPMI-8226/ScellsConcentration:0-10μMIncubationTime:3daysResult:InhibitedMMcelllinesincludingAMO-1,ARH-77,IM-9,JJN-3,L-363,MOLP-8andRPMI-8226/ScellswithGI50svof3.23,4.31,4.87,2.56,4.64,4.67and3.97μM,respectively.WesternBlotAnalysis[3]CellLine:MM(S)andmelphalan-resistant(LR5)MMcellsConcentration:5μMIncubationTime:16hoursResult:AbolishedmelphalaninducedFANCD2mono-ubiquitinationandDNAdamageinLR5,sensitizedLR5tomelphalan-inducedcelldeathbyblockingFANCD2-mediatedDNAdamagerepair.ApoptosisAnalysis[3]CellLine:Bortezomib-resistantMMpatientscellsConcentration:5μM2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIncubationTime:2daysResult:2-foldincreasedcellapoptosisinthecellderivedfrombortezomib-resistantMMpatients.体内研究CASIN(20mg/kg;i.p.2timesaday)prolongslifetimeofmicewithbusulfaninjection[1].AnimalModel:NSGmicewithbusulfaninjection[3]Dosage:20mg/kgAdministration:Intraperitonealinjection;20mg/kg2timesadayResult:Significantlyprolongedthelifespanofxenograftsmicebetterthanbortezomib,andshowedaleadingpositionwhencombinedwithbortezomib.户使⽤本产品发表的科研⽂献•NatCommun.2022Nov11;13(1):6840.•ClinTranslMed.2022Jun;12(6):e850.•EcotoxicolEnvironSaf.2022Jan17;231:113208.•ToxicolSci.2018Sep1;165(1):254-266.•BirthDefectsRes.2020Dec10.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].NguyenP,etal.RationalTargetingofCdc42OvercomesDrugResistanceofMultipleMyeloma.FrontOncol.2019Oct1;9:958.doi:10.3389/fonc.2019.00958.[2].FlorianMCetal.Cdc42activityregulateshematopoieticstemcellagingandrejuvenation.CellStemCell,2012May4,10(5):520-30.McePdfHeightCaution:Producthasnot