Adipogen/AGI-5198/AG-CR1-3528-M005/5 mg
商品编号：
AG-CR1-3528-M005
品牌：
Adipogen Inc
市场价：
¥1600.00
美元价：
960.00
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
| ProductDetails | |
|---|---|
| Synonyms | N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-imidazole-1-acetamide;IDH-C35 |
| ProductType | Chemical |
| Properties | |
| Formula | C27H31FN4O2 |
| MW | 462.6 |
| CAS | 1355326-35-0 |
| PurityChemicals | ≥98%(NMR) |
| Appearance | Whitesolid. |
| Solubility | SolubleinDMSO(10mg/ml)orethanol(5mg/ml). |
| Identity | Determinedby1H-NMR. |
| InChiKey | FNYGWXSATBUBER-UHFFFAOYSA-N |
| ShippingandHandling | |
| Shipping | AMBIENT |
| ShortTermStorage | +4°C |
| LongTermStorage | -20°C |
| HandlingAdvice | Keepcoolanddry. |
| Use/StABIlity | Stableforatleast2yearsafterreceiptwhenstoredat-20°C. |
| Documents | |
| MSDS |  DownloadPDF |
| ProductSpecificationSheet | |
| Datasheet | DownloadPDF |
- 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
- Cancer-associatedIDH1mutationsproduce2-hydroxyglutarate:L.Dang,etal.;Nature462,739(2009)
- Transformationbythe(R)-enantiomerof2-hydroxyglutaratelinkedtoEGLNactivation:P.Koivunen,etal.;Nature483,484(2012)
- IDH1mutationissufficienttoestablishthegliomahypermethylatorphenotype:S.Turcan,etal.,Nature483,479(2012)
- Isocitratedehydrogenase1and2mutationsincancer:alterationsatacrossroadsofcellularmetabolism:Z.J.Reitman&H.Yan;J.Natl.CancerInst.102,932(2010)
- DiscoveryofthefirstpotentinhibitorsofmutantIDH1thatlowertumor2-HGinvivo:J.Popovici-Muller,etal.;ACSMed.Chem.Lett.3,850(2012)
- 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。
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