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Ingenol Mebutate

Cat. No.:YN310337

  • CAS No. :75567-37-2

    • 产品资料
    • 生物活性
    • 参考文献
    • 产品名称: Ingenol Mebutate
      CAS No.: 75567-37-2
      Chemical Name: 2Z-methyl-2-butenoic acid, (1aR,2S,5R,5aS,6S,8aS,9R,10aR)-1a,2,5,5a,6,9,10,10a-octahydro-5,5a-dihydroxy-4-(hydroxymethyl)-1,1,7,9-tetramethyl-11-oxo-1H-2,8a-methanocyclopenta[a]cyclopropa[e]cyclodecen-6-yl ester
      Synonyms:巨大戟醇甲基丁烯酸酯; Ingenol 3-angelate; PEP005
      分子量:430.53
      分子式:C₂₅H₃₄O₆
      SMILES:C/C=C(C)\C(O[C@H]1C(C)=C[C@]23[C@]1(O)[C@H](O)C(CO)=C[C@@](C3=O)([H])[C@@]4([H])[C@@](C4(C)C)([H])C[C@H]2C)=O
      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: Ingenol Mebutate 是Euphorbia peplus中的活性成分,为PKC的调节剂,对 PKC-α,PKC-β,PKC-γ,PKC-δ 和 PKC-ε 的Ki值分别为 0.3,0.105,0.162,0.376 和 0.171 nM。
      IC50和靶点: [{name:"PKC-β:0.105 nM (Ki)"},{name: "PKC-γ:0.162 nM (Ki)"},{name: "PKC-ε:0.171 nM (Ki)"},{name: "PKC-α:0.3 nM (Ki)"},{name: "PKC-δ:0.376 nM (Ki)"}]
      In Vitro:
      In Vivo:
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    • Ogbourne, S.M., Suhrbier, A., Jones, B., et al.Antitumor activity of 3-ingenyl angelate: Plasma membrane and mitochondrial disruption and necrotic cell deathCancer Res.64(8),2833-2839(2004)

      Gillespie, S.K., Zhang, X.D., and Hersey, P.Ingenol 3-angelate induces dual modes of cell death and differentially regulates tumor necrosis factor-related apoptosis-inducing ligand-induced apoptosis in melanoma cellsMol. Cancer Ther.3(12),1651-1658(2004)

      Li, L., Shukla, S., Lee, A., et al.The skin cancer chemotherapeutic agent ingenol-3-angelate (PEP005) is a substrate for the epidermal multidrug transporter (ABCB1) and targets tumor vasculatureCancer Res.70(11),4509-4519(2010)

      Hasler, C.M., Acs, G., and Blumberg, P.M.Specific binding to protein kinase C by ingenol and its induction of biological responsesCancer Res.52(1),202-208(1992)

      Lebwohl, M., Swanson, N., Anderson, L.L., et al.Ingenol mebutate gel for actinic keratosisN. Engl. J. Med.366(11),1010-1019(2012)

      Micali, G., Lacarrubba, F., Nasca, M.R., et al.Topical pharmacotherapy for skin cancer. Part I. PharmacologyJ. Am. Acad. Dermatol.70(6),965.e961-956.e912(2014)

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