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当前位置: 首页 > 产品中心 > Other_reagents > Adipogen/Delanzomib [CEP-18770]/AG-CR1-3673-M001/1 mg
商品详细Adipogen/Delanzomib [CEP-18770]/AG-CR1-3673-M001/1 mg
Adipogen/Delanzomib [CEP-18770]/AG-CR1-3673-M001/1 mg
Adipogen/Delanzomib [CEP-18770]/AG-CR1-3673-M001/1 mg
商品编号: AG-CR1-3673-M001
品牌: Adipogen Inc
市场价: ¥800.00
美元价: 480.00
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
SynonymsNPH007098;CT47098;CIP18770;[(1R)-1-[[(2S,3R)-3-Hydroxy-2-[(6-phenylpyridine-2-carbonyl)amino]butanoyl]amino]-3-methylbutyl]boronicacid
ProductTypeChemical
Properties
FormulaC21H28BN3O5
MW413.3
CAS847499-27-8
PurityChemicals≥98%
AppearanceWhitesolid.
SolubilitySolubleinDMSO(20mg/ml)orethanol(20mg/ml).Slightlysolubleinchloroformormethanol.Poorlysolubleinwater(<1mg l).="">
OtherProductDataNote:Warmingandsonicationmayberequiredwhendissolvingthecompoundinthesolventofchoice.Stocksolutionsarestableforatleast1monthwhenstoredat-20°C.
InChiKeySJFBTAPEPRWNKH-CCKFTAQKSA-N
ShippingandHandling
ShippingAMBIENT
ShortTermStorage+4°C
LongTermStorage-20°C
HandlingAdviceKeepcoolanddry.
Use/StABIlityStableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDSDownloadPDF
ProductSpecificationSheet
DatasheetDownloadPDF
  • Potent,selective,reversIBLeorallybioavailableproteasomeinhibitor.SyntheticP2threonineboronicacid.
  • Targetsthechymotrypsin-likeβ5subunitoftheconstitutive20Sproteasome(IC50=3.8nM).Cross-reactsandinhibitsthecaspase-like/peptidyl-glutamylpeptide-hydrolyzing(PGPH)β1subunit(IC50=~70nM).
  • Displayssimilarpotencyforthechymotrypsin-likeactivityoftheproteasomecomparedtobortezomib.Exhibitsafavorablecytotoxicityprofiletowardnormalhumanepithelialcells,bonemarrowProgenitorsandbonemarrow-derivedstromalcellsrelativetobortezomib(Prod.No.AG-CR1-3602).
  • Anticancercompoundeffectiveagainstmultiplemyelomainvivo.
  • Invitro,blocksthegrowthofrepresentativehumansolidandhematologicaltumorcelllines(IC50s=5.6-34nM).
  • Showntodown-modulateNF-κB,induceapoptosis,inhibitangiogenesisandM-CSF-RANKL-inducedosteoclastogenesis.
ProductReferences
  1. DiscoveryofaPotent,Selective,andOrallyActiveProteasomeInhibitorfortheTreatmentofCancer:B.D.Dorsey,etal.;J.Med.Chem.51,1068(2008)
  2. CEP-18770:Anovel,orallyactiveproteasomeinhibitorwithatumor-selectivepharmacologicprofilecompetitivewithbortezomib:R.Piva,etal.;Blood111,2765(2008)
  3. TheproteasomeinhibitorCEP-18770enhancestheanti-myelomaactivityofbortezomibandmelphalan:E.Sanchez,etal.;Br.J.Haematol.148,569(2010)
  4. Novel,orallyactive,proteasomeinhibitor,delanzomib(CEP-18770),amelioratesdiseasesymptomsandglomerulonephritisintwopreclinicalmousemodelsofSLE:M.M.Seavey,etal.;Int.Immunopharmacol.12,257(2012)
  5. Probingthespecificityandactivityprofilesoftheproteasomeinhibitorsbortezomibanddelanzomib:C.R.Berkers,etal.;Mol.Pharm.9,1126(2012)
  6. Molecularmechanismsofacquiredproteasomeinhibitorresistance:A.J.Kale&B.S.Moore;J.Med.Chem.55,10317(2012)
  7. AfirstinhumanphaseIstudyoftheproteasomeinhibitorCEP-18770inpatientswithadvancedsolidtumoursandmultiplemyeloma:E.Gallerani,etal.;Eur.J.Cancer49,290(2013)
  8. Proteasomeinhibitorsinthetreatmentofmultiplemyeloma:A.McBride&P.Y.Ryan;ExpertRev.AnticancerTher.13,339(2013)(Review)
  9. PhaseI/IIstudyofthenovelproteasomeinhibitordelanzomib(CEP-18770)forrelapsedandrefractorymultiplemyeloma:D.T.Vogl,etal.;Leuk.Lymphoma58,1872(2017)
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。