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当前位置: 首页 > 产品中心 > Other_reagents > Adipogen/A-674563 (free base)/AG-CR1-3680-M010/10 mg
商品详细Adipogen/A-674563 (free base)/AG-CR1-3680-M010/10 mg
Adipogen/A-674563 (free base)/AG-CR1-3680-M010/10 mg
Adipogen/A-674563 (free base)/AG-CR1-3680-M010/10 mg
商品编号: AG-CR1-3680-M010
品牌: Adipogen Inc
市场价: ¥4200.00
美元价: 2520.00
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
SynonymsαS-[[[5-(3-Methyl-1H-indazol-5-yl)-3-pyridinyl]oxy]methyl]-benzeneethanamine
ProductTypeChemical
Properties
Formula

C22H22N4O

MW358.4
CAS552325-73-2
PurityChemicals≥98%(HPLC)
AppearanceWhitetooff-whitesolid.
SolubilitySolubleinDMF(20mg/ml),DMSO(10mg/ml)orethanol(10mg/ml).
InChiKeyBPNUQXPIQBZCMR-IBGZPJMESA-N
ShippingandHandling
ShippingAMBIENT
ShortTermStorage+4°C
LongTermStorage-20°C
HandlingAdviceKeepcoolanddry.
Use/StABIlityStableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDSDownloadPDF
ProductSpecificationSheet
DatasheetDownloadPDF
  • A-674563isapotent,ATP-competitive,reversIBLeandorallyavailableAkt1inhibitorwithanIC50of11nM.BindstotheATPsiteoftheAKTkinasedomain,inhibitingAKT-catalyzedphosphorylationactivity.
  • AlsoinhibitsPKAandCDK2withIC50valuesof16nMand46nM,respectively.
  • 10-to>1,800-foldselectiveforAkt1versusadditionalkinasesintheCMGC,CAMKandTKfamilies.
  • Anticancercompound.ReducesphosphorylationofAktdownstreamtargetsincellsandslowsproliferationoftumorcellsinvitrowithanEC50valueof0.4µM.
  • Showntodecreasetumorgrowthinmousetumorxenograftmodels.
  • Decreasedsphingosinekinase1(SphK1)activityinAMLcellstodepletepro-survivalsphingosine-1-phosphate(S1P)andboostpro-apoptoticceramideproduction.
ProductReferences
  1. PotentandselectiveinhibitorsofAktkinasesslowtheprogressoftumorsinvivo:Y.Luo,etal.;Mol.CancerTher.4,977(2005)
  2. CharacterizationofanAktkinaseinhibitorwithpotentpharmacodynamicandantitumoractivity:N.Rhodes,etal.;CancerRes.68,2366(2008)
  3. SofttissuesarcomacellsarehighlysensitivetoAKTblockade:aroleforp53-independentup-regulationofGADD45alpha:Q.S.Zhu,etal.;CancerRes.68,2895(2008)
  4. EnhancedsensitivitytosorafenibbyinhibitionofAkt1expressioninhumanrenalcellcarcinomaACHNcellsbothinvitroandinvivo:H.Tei,etal.;Hum.Cell.28,114(2015)
  5. UniquerolesofAkt1andAkt2inIGF-IRmediatedlungtumOrigenesis:S.E.Franks,etal.;Oncotarget7,3297(2016)
  6. DualinhibitionofAKT/FLT3-ITDbyA674563overcomesFLT3ligand-induceddrugresistanceinFLT3-ITDpositiveAML:A.Wang,etal.;Oncotarget7,29131(2016)
  7. ConcurrenttargetingAktandsphingosinekinase1byA-674563inacutemyeloidleukemiacells:L.Xu,etal.;BBRC472,662(2016)
  8. Pre-clinicalassessmentofA-674563asananti-melanomaagent:Y.Zou,etal.;BBRC477,1(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。