Nilotinib-AMN107-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENilotinibCat.No.:HY-10159CASNo.:641571-10-0Synonyms:AMN107分⼦式:C₂₈H₂₂F₃N₇O分⼦量:529.52作⽤靶点:Bcr-Abl;Autophagy作⽤通路:ProteinTyrosineKinase/RTK;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:<1mg/mL(ultrasonic;warming;heatto60°C)(insolubleorslightlysoluble)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%salineSolubility:≥0.6mg/mL(1.13mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.6mg/mL(1.13mM);Suspendedsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥0.6mg/mL(1.13mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE⽣物活性Nilotinib⼀种⼝服可⽤的具有抗肿瘤活性的Bcr-Abl酪氨酸激酶抑制剂。IC50&TargetBcr-Abl[1]体外研究Nilotinib(AMN107),selectiveAblinhibitor,isdesignedtointeractwiththeATP-bindingsiteofBCR-ABLwithahigheraffinitythanimatinibwhilebeingsignificantlymorepotentcomparedwithimatinib(IC50[1].NilotinibdemonstratessignificantantitumorefficacyagainstGISTxenograftlinesandimatinib-resistantGISTcelllineswhichparentcelllinesGK1CandGK3CshowsimatinibsensitivitywithIC50of4.59±0.97µMand11.15±1.48µM,respectively,imatinib-resistantcelllinesGK1C-IRandGK3C-IRshowsImatinibresistancewithIC50valuesof11.74±0.17µM(P[2].体内研究Nilotinib(oralgavage,40mg/kg,daily,4weeks)showsequivalentorhigherantitumoreffectsinBALB/cSLc-nu/numicewithGISTxenograft[2].Nilotinibhasasignificanthealingeffectonthemacroscopicandmicroscopicpathologicscoresandensuresconsiderablemucosalhealingintheindomethacin-inducedenterocolitisratmodelwhiledecreasesthePDGFRαandβlevelsandapoptoticscoresinthecolon[3].AnimalModel:BALB/cSLc-nu/numicewithGISTxenograft(GK1X,GK2XandGK3X)[2]Dosage:40mg/kgAdministration:Oralgavage;daily;4weeksResult:Inhibitedtumorgrowthby69.6%inGK1X,85.3%inGK2Xand47.5%inGK3Xxenograftline.户使⽤本产品发表的科研⽂献•SciTranslMed.2018Jul18;10(450).pii:eaaq1093.•Biomaterials.16September2022.•CellSyst.2018Apr25;6(4):424-443.e7.•BrJCancer.2021Nov24.•CellDeathDis.2021Sep25;12(10):875.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].WeisbergE,etal.BeneficialeffectsofcombiningnilotinibandimatinibinpreclinicalmodelsofBCR-ABL+leukemias.Blood.2007Mar1;109(5):2112-20.[2].SakoH,etal.AntitumoreffectofthetyrosinekinaseinhibitorNilotinibongastrointestinalstromaltumor(GIST)andImatinib-resistantGISTcells.PLoSOne.2014Sep15;9(9):e107613.[3].DervisHakimG,etal.Mucosalhealingeffectofnilotinibinindomethacin-inducedenterocolitis:Aratmodel.WorldJGastroenterol.2015Nov28;21(44):12576-85.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[4].FujitaKI,etal.InvolvementoftheTransportersP-GlycoproteinandBreastCancerResistanceProteininDermalDistributionoftheMultikinaseInhibitorRegorafenibandItsActiveMetabolites.JPharmSci.2017Sep;106(9):2632-2641.[5].MeirsonT,etal.Targetinginvadopodia-mediatedbreastcancermetastasisbyusingABLkinaseinhibitors.Oncotarget.2018Apr24;9(31):22158-22183.McePdfHeightCaution:Product