Nilotinib-AMN107-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENilotinibCat.No.:HY-10159CASNo.:641571-10-0Synonyms:AMN107分?式:C??H??F?N?O分?量:529.52作?靶點:Bcr-Abl;Autophagy作?通路:ProteinTyrosineKinase/RTK;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:<1mg/mL(ultrasonic;warming;heatto60°C)(insolubleorslightlysoluble)請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥0.6mg/mL(1.13mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥0.6mg/mL(1.13mM);Suspendedsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥0.6mg/mL(1.13mM);ClearsolutionBIOLOGICALACTIVITY1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE?物活性Nilotinib?種?服可?的具有抗腫瘤活性的Bcr-Abl酪氨酸激酶抑制劑。IC50&TargetBcr-Abl[1]體外研究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].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師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