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I-BET151

Cat. No.:YN310211

  • CAS No. :1300031-49-5

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    • 参考文献
    • 产品名称: I-BET151
      CAS No.: 1300031-49-5
      Chemical Name: 7,3,5-dimethyl-4-isoxazolyl-1,3-dihydro-8-methoxy-1-[1R-1-(2-pyridinyl)ethyl]-2H-imidazo[4,5-c]quinolin-2-one
      Synonyms:GSK1210151A
      分子量:415.44
      分子式:C₂₃H₂₁N₅O₃
      SMILES:C[C@@H](N1C(C(C=C(OC)C(C2=C(C)ON=C2C)=C3)=C3N=C4)=C4NC1=O)C5=CC=CC=N5
      存储:Please store the product under the recommended conditions in theCertificate of Analysis.
      运输:Room temperature in continental US; may vary elsewhere.
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      Purity: 98%
    • 产品描述: I-BET151 是一种 BET溴结构域 (BET bromodomain) 抑制剂,抑制BRD4,BRD2和BRD3的pIC50分别为 6.1,6.3 和 6.6。
      IC50和靶点:
      In Vitro:
      In Vivo:
      Clinical Trial:
      Solvent & Solubility:
    • Gallenkamp, D., Gelato, K.A., Haendler, B., et al.Bromodomains and their pharmacological inhibitorsChem. Med. Chem.9(3),438-464(2014)

      Kline, T.B., Benington, F., Morin, R.D., et al.Structure-activity relationships for hallucinogenic N,N-dialkyltryptamines: Photoelectron spectra and serotonin receptor affinities of methylthio and methylenedioxy derivativesJ. Med. Chem.25(11),1381-1383(1982)

      Vidler, L.R., Brown, N., Knapp, S., et al.Druggability analysis and structural classification of bromodomain acetyl-lysine binding sitesJ. Med. Chem.55(17),7346-7359(2012)

      Hewings, D.S., Fedorov, O., Filippakopoulos, P., et al.Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligandsJ. Med. Chem.56(8),3217-3227(2013)

      Dawson, M.A., Kouzarides, T., and Huntly, B.J.Targeting epigenetic readers in cancerN. Engl. J. Med.367(7),647-657(2012)

      Dawson, M.A., Prinjha, R.K., Dittmann, A., et al.Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemiaNature478,529-533(2011)

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