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PIK-75 hydrochloride

Cat. No.:YN420158

  • CAS No. :372196-77-5

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    • 产品名称: PIK-75 hydrochloride
      CAS No.: 372196-77-5
      Chemical Name: 2-methyl-5-nitro-2-[(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-1-methylhydrazide-benzenesulfonic acid, monohydrochloride
      Synonyms:PIK-75 HCl,2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-a]吡啶-3-基)亚甲基]甲基肼盐酸盐,PIK-75
      分子量:488.74
      分子式:C₁₆H₁₅BrClN₅O₄S
      SMILES:BrC(C=C1)=CN2C1=NC=C2/C=N/N(S(=O)(C3=C(C=CC([N+]([O-])=O)=C3)C)=O)C.[H]Cl
      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: PIK-75 hydrochloride 是一种可逆的DNA-PK和p110α-选择性的抑制剂,抑制 DNA-PK,p110α和 p110γ,IC50分别为 2,5.8 和 76 nM。PIK-75 hydrochloride 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。PIK-75 hydrochloride 诱导凋亡 (apoptosis)。
      IC50和靶点: [{name:"DNA-PK:2 nM (IC50)"},{name: "p110α:5.8 nM (IC50)"},{name: "p110γ:76 nM (IC50)"},{name: "p110δ:510 nM (IC50)"},{name: "p110β:1.3 μM (IC50)"},{name: "hsVPS34:2.6 μM (IC50)"},{name: "PI3KC2β:1 μM (IC50)"},{name: "PI3KC2α:10 μM (IC50)"},{name: "mTORC1:1 μM (IC50)"},{name: "mTORC2:10 μM (IC50)"},{name: "ATM:2.3 μM (IC50)"},{name: "ATR:21 μM (IC50)"},{name: "PI4KIIIβ:50 μM (IC50)"}]
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    • Fan, Q.W., Knight, Z.A., Goldenberg, D.D., et al.A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in gliomaCancer Cell9(5),341-349(2006)

      Knight, Z.A., Gonzalez, B., Feldman, M.E., et al.A pharmacological map of the PI3-K family defines a role for p110α in insulin signalingCell125(4),733-747(2006)

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