Teglarinad-chloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesTeglarinadchlorideCat.No.:HY-10080CASNo.:432037-57-5分⼦式:C₃₀H₄₃Cl₂N₅O₈分⼦量:672.6作⽤靶点:NAMPT作⽤通路:MetabolicEnzyme/Protease储存⽅式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)溶解性数据体外实验DMSO:200mg/mL(297.35mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4868mL7.4338mL14.8677mL5mM0.2974mL1.4868mL2.9735mL10mM0.1487mL0.7434mL1.4868mL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，并请注意储备液的保存⽅式和期限。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%DMSO40%PEG3005%Tween-8045%salineSolubility:≥5mg/mL(7.43mM);Clearsolution此⽅案可获得≥5mg/mL(7.43mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL50.0mg/mL的澄DMSO储备液加到400μLPEG300中，混合均匀；向上述2.体系中加⼊50μLTween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。请依序添加每种溶剂：10%DMSO90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(7.43mM);Clearsolution1/3此⽅案可获得≥5mg/mL(7.43mM，饱和度未知)的澄溶液。以1mL⼯作液为例，取100μL50.0mg/mL的澄DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶3.液中，混合均匀。请依序添加每种溶剂：10%DMSO90%cornoilSolubility:≥5mg/mL(7.43mM);Clearsolution此⽅案可获得≥5mg/mL(7.43mM，饱和度未知)的澄溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。以1mL⼯作液为例，取100μL50.0mg/mL的澄DMSO储备液加到900μL⽟⽶油中，混合均匀。BIOLOGICALACTIVITY⽣物活性Teglarinadchloride(GMX1777)GMX1778(⼀种烟酰胺磷酸核糖转移酶抑制剂)的前药。Teglarinadchloride在⼩⿏中表现出抗肿瘤活性可以归因于NAMPT的抑制。Teglarinadchloride通过⼲扰DNA修复和抗⾎管⽣成，可以增强放射功效。体内研究GMX1777(75mg/kg;24hintravenousinfusion)causestumorregressionintheIM-9model,asmall-celllungcancer(SHP-77)model,andacoloncarcinoma(HCT-116)model[2].GMX1777(50-100mg/kg/d,i.m.for5d)withorwithoutlocaltumorradiotherapyiseffectiveforbothFaDuandC666-1tumorsinvivo[1].GMX1777(25-400mg/kg;24hintravenousinfusion)isquicklyconvertedtoGMX1778inplasmaofmicewithahalf-lifeofGMX1777lessthan0.7h[2].AnimalModel:CB17SCID/SCIDfemalemicebearingsubcutaneousIM-9multiplemyelomatumors[2]Dosage:18.75,35,75mg/kgAdministration:A24hintravenousinfusionResult:Inducedanearlycompleteregressionofthetumorsandasignificanttumorgrowthdelayatthedoseof75mg/kg.ReducedIM-9tumorgrowthmoderatelyat37.5mg/kg.REFERENCES[1].KatoH,et,al.EfficacyofcombiningGMX1777withradiationtherapyforhumanheadandneckcarcinoma.ClinCancerRes.2010Feb1;16(3):898-911.[2].BeauparlantP,et,al.PreclinicaldevelopmentofthenicotinamidephosphoribosyltransferaseinhibitorprodrugGMX1777.AnticancerDrugs.2009Jun;20(5):346-54.McePdfHeight2/3MedChemExpres