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当前位置: 首页 > 产品中心 > Other_reagents > 脂肪原/AGI-5198/AG-CR1-3528-M025/25毫克
商品详细脂肪原/AGI-5198/AG-CR1-3528-M025/25毫克
脂肪原/AGI-5198/AG-CR1-3528-M025/25毫克
脂肪原/AGI-5198/AG-CR1-3528-M025/25毫克
商品编号: AG-CR1-3528-M025
品牌: Adipogen Inc
市场价: ¥4800.00
美元价: 2880.00
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
SynonymsN-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide;IDH-C35
ProductTypeChemical
Properties
FormulaC27H31FN4O2
MW462.6
CAS1355326-35-0
PurityChemicals≥98%(NMR)
AppearanceWhitesolid.
SolubilitySolubleinDMSO(10mg/ml)orethanol(5mg/ml).
IdentityDeterminedby1H-NMR.
InChiKeyFNYGWXSATBUBER-UHFFFAOYSA-N
ShippingandHandling
ShippingAMBIENT
ShortTermStorage+4°C
LongTermStorage-20°C
HandlingAdviceKeepcoolanddry.
Use/StABIlityStableforatleast2yearsafterreceiptwhenstoredat-20°C.
Documents
MSDSDownloadPDF
ProductSpecificationSheet
DatasheetDownloadPDF
  • PotentandselectiveinhibitorofIDH1(isocitratedehydrogenase1)R132HandR132CmutantsinvitrowithIC50valuesof0.07and0.16µM,respectively.Doesnotinhibitwild-typeIDH1oranyoftheexaminedIDH2isoforms(IC50>100µM).Isocitratedehydrogenases(IDHs)arenicotinamideadeninedinucleotide(NAD+)andNADphosphate(NADP+)-dependentenzymesinthetricarboxylicacidcyclethatcatalyzeoxidativedecarboxylationofisocitrateproducingα-ketoglutarate(2-OG)andcarbondioxide.IDH1andIDH2aremutatedin>70%oflowergradegliomas.
  • Showntohaveanti-tumorefficacyintheTS603gliomacelllineandtoreducetumor2-HGproductioninHT1080andU87MGcells.
  • Caused50-60%growthinhibitionoveratreatmentperiodofthreeweekswithnoaffectinthegrowthofIDH1wild-typegliomaxenograftsinR132H-IDH1gliomaxenografts.
  • Underconditionsofnearcomplete2-HGinhibition,inducesdemethylationofhistoneH3K9me3andexpressionofgenesassociatedwithgliogenicdifferentiation.
  • UsefulchemicalprobetoassesstheBIOLOGicalconsequencesofIDH1mutationsandthepotentialofIDH1inhibitionfortreatingIDH1mutanttumors.
  • Requireshighdosesforinvivoactivity,butcanbeusedthroughoraldosingroute.
ProductReferences
  1. Cancer-associatedIDH1mutationsproduce2-hydroxyglutarate:L.Dang,etal.;Nature462,739(2009)
  2. Transformationbythe(R)-enantiomerof2-hydroxyglutaratelinkedtoEGLNactivation:P.Koivunen,etal.;Nature483,484(2012)
  3. IDH1mutationissufficienttoestablishthegliomahypermethylatorphenotype:S.Turcan,etal.,Nature483,479(2012)
  4. Isocitratedehydrogenase1and2mutationsincancer:alterationsatacrossroadsofcellularmetabolism:Z.J.Reitman&H.Yan;J.Natl.CancerInst.102,932(2010)
  5. DiscoveryofthefirstpotentinhibitorsofmutantIDH1thatlowertumor2-HGinvivo:J.Popovici-Muller,etal.;ACSMed.Chem.Lett.3,850(2012)
  6. AninhibitorofmutantIDH1delaysgrowthandpromotesdifferentiationofgliomacells:D.Rohle,etal.;Science340,626(2013)
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。