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当前位置: 首页 > 产品中心 > Other_reagents > Adipogen/CX-4945 . hydrochloride/AG-CR1-3629-M005/5 mg
商品详细Adipogen/CX-4945 . hydrochloride/AG-CR1-3629-M005/5 mg
Adipogen/CX-4945 . hydrochloride/AG-CR1-3629-M005/5 mg
Adipogen/CX-4945 . hydrochloride/AG-CR1-3629-M005/5 mg
商品编号: AG-CR1-3629-M005
品牌: Adipogen Inc
市场价: ¥3300.00
美元价: 1980.00
产地: 美国(厂家直采)
公司:
产品分类: 其他试剂
公司分类: Other_reagents
联系Q Q: 3392242852
电话号码: 4000-520-616
电子邮箱: info@ebiomall.com
商品介绍
MoreInformation
ProductDetails
SynonymsSilmitasertib.HCl;8-Carboxy-N-(3-chlorophenyl)benzo[c][2,6]naphthyridin-5-aminiumchloride
ProductTypeChemical
Properties
FormulaC19H12ClN3O2.HCl
MW349.8.36.5
CAS1009820-21-6(freeacid)
PurityChemicals≥98%
AppearanceYellowsolid.
SolubilitySolubleinDMSO.Insolubleinwater.
InChiKeyOBOIGMDUOMSAHW-UHFFFAOYSA-N
ShippingandHandling
ShippingAMBIENT
ShortTermStorage+4°C
LongTermStorage-20°C
HandlingAdviceKeepcoolanddry.
Use/StABIlityStableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDSDownloadPDF
ProductSpecificationSheet
DatasheetDownloadPDF
  • Orallyactive,potentandselectiveATP-competitiveinhibitoroftheproteinkinaseCK2(IC50=1nM).
  • Anticancercompound.InhibitsproliferationinapanelofcancercelllinesthatoverexpressCK2.Inhibitedmigration,blockssurvivalandinducesapoptosisincancerstemcells,glioblastomasandleukemiacells.
  • Showntodecreasetheglucosemetabolismincancercells.
  • PotentinhibitorofCdc2-likekinases(Clks)invitro,consequentlyinterferingwithalternativesplicing.
  • PotentATP-competitiveinhibitorofDYRK1A(IC50=6.8nM),DYRK1B(IC50=6.4nM)andDYRK3(IC50=18nM),involvedinneurodegeneration-associateddiseases.
  • CK2αdeletionselectivelyincreasedM3muscarinicreceptors(M3Rs)-mediatedinsulinsecretionfrompancreaticislets.
  • PromotedcAMP-inducedThermogenesisinwhiteADIpocytes.
  • CK2inhibitionamelioratesdiet-inducedobesityandinsulinresistanceinmiceinvivobypromotingUCP1-dependentthermogenesis.
ProductReferences
  1. CX-4945,anorallybioavailableselectiveinhibitorofproteinkinaseCK2,inhibitsprosurvivalandangiogenicsignalingandexhibitsantitumorefficacy:A.Siddiqui-Jain,etal.;CancerRes.70,10288(2010)
  2. StructuralbasisofCX-4945bindingtohumanproteinkinaseCK2:A.D.Ferguson,etal.;FEBSLett.585,104(2011)
  3. DiscoveryandSARof5-(3-chlorophenylamino)benzo[c][2,6]naphthyridine-8-carboxylicacid(CX-4945),thefirstclinicalstageinhibitorofproteinkinaseCK2forthetreatmentofcancer:F.Pierre,etal.;J.Med.Chem.54,635(2011)
  4. Pre-clinicalcharacterizationofCX-4945,apotentandselectivesmallmoleculeinhibitorofCK2forthetreatmentofcancer:F.Pierre,etal.;Mol.CellBiochem.356,37(2011)
  5. CX-4945,aselectiveinhibitorofcaseinkinase-2(CK2),exhibitsanti-tumoractivityinhematologicmalignanciesincludingenhancedactivityinchroniclymphocyticleukemiawhencombinedwithfludarabineandinhibitorsoftheB-cellreceptorpathway:R.C.Prins,etal.;Leukemia27,2094(2013)
  6. CK2inhibitorCX4945inducessequentialinactivationofproteinsinthesignalingpathwaysrelatedwithcellmigrationandsuppressesmetastasisofA549humanlungcancercells:M.J.Ku,etal.;Bioorg.Med.Chem.Lett.23,5609(2013)
  7. IdentificationofanovelfunctionofCX-4945asasplicingregulator:H.Kim,etal.;PLosOne9,e94978(2014)
  8. Activityoftheclinical-stageCK2-specificinhibitorCX-4945againstchroniclymphocyticleukemia:L.R.Martins,etal.;Leukemia28,179(2014)
  9. PhosphoproteomicsidentifiesCK2asanegativeregulatorofbeigeadipocytethermogenesisandenergyexpenditure:K.Shinoda,etal.;CellMetab.22,997(2015)
  10. CK2actsasapotentnegativeregulatorofreceptor-mediatedinsulinreleaseinvitroandinvivo:M.Rossi,etal.;PNAS112,E6818(2015)
  11. Thecaseinkinase2inhibitor,CX-4945,asananti-cancerdrugintreatmentofhumanhematologicalmalignancies:H.J.Chon,etal.;Front.Pharmacol.6,70(2015)
  12. AchemicalwithprovenclinicalsafetyrescuesDown-syndrome-relatedphenotypesinthroughDYRK1Ainhibition:H.Kim,etal.;Dis.ModelMech.9,839(2016)
  13. TargetingproteinkinaseCK2suppressesbladdercancercellsurvivalviatheglucosemetabolicpathway:X.Zhang,etal.;Oncotarget7,87361(2016)
品牌介绍
Adipogen公司由三个子公司组成,分别是Adipogen,Inc.(韩国),AdipogenSA(瑞士)和 AdipogenCorporation(美国圣地亚哥)。总部设在美国,运营总部在瑞士利斯塔尔。Adipogen公司专门从事生命科学研究试剂的开发,如癌症、免疫、炎症、代谢疾病(糖尿病、肥胖)、干细胞和神经退行性疾病等领域。其重点关注开发创新优质的ELISA试剂盒。另外,也可提供抗体和蛋白产品,Adipogen拥有自己的化学实验室,致力于开发创新型小分子化合物。