GGTI-2154-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEGGTI-2154hydrochlorideCat.No.:HY-16229ACASNo.:478908-50-8分⼦式:C₂₄H₂₉ClN₄O₃分⼦量:456.97作⽤靶点:ROS;Apoptosis作⽤通路:ProteinTyrosineKinase/RTK;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:250mg/mL(547.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1883mL10.9416mL21.8833mL5mM0.4377mL2.1883mL4.3767mL10mM0.2188mL1.0942mL2.1883mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥25mg/mL(54.71mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥25mg/mL(54.71mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥25mg/mL(54.71mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性GGTI-2154hydrochloride⼀种有效和选择性的geranylgeranyltransferaseI(GGTaseI)抑制剂，IC50值为21nM。GGTI-2154hydrochloride对GGTaseI的选择性FTase(IC50=5600nM)的200倍以上。GGTI-2154hydrochloride可⽤于癌症的研究。IC50&TargetIC50:21nM(GGTaseI)[1]体外研究GGTI-2154inhibitsthetransferofgeranylgeranylfrom[3H]GGPPtoH-RasCVLL,withanIC50of21nM[1].体内研究GGTI-2154(100mg/kg/day;s.c.for14days)inducesbreasttumorregressioninMMTV-ν-Ha-Rastransgenicmice[2].GGTI-2154(50mg/kg/day;i.p.for50day)inhibitsA-549tumorgrowthinnudemiceby60%[1].AnimalModel:MMTV-v-Ha-rastransgenicmicebearingmammarycarcinoma[2]Dosage:100mg/kg/dayAdministration:S.c.withosmoticmini-pumpsfor14daysResult:Haltedthetumorsaggressivegrowth.Resultedinrapidtumorregressionwithin3daysofinitiationofdrugtreatment.REFERENCES[1].SunJ,et,al.Antitumorefficacyofanovelclassofnon-thiol-containingpeptidomimeticinhibitorsoffarnesyltransferaseandgeranylgeranyltransferaseI:combinationtherapywiththecytotoxicagentscisplatin,Taxol,andgemcitabine.CancerRes.1999Oct1;59(19):4919-26.[2].SunJ,et,al.GeranylgeranyltransferaseIinhibitorGGTI-2154inducesbreastcarcinomaapoptosisandtumorregressioninH-Rastransgenicmice.CancerRes.2003Dec15;63(24):8922-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicatio