RG-120086 | 748155-63-7

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: RG-120086
• 英文别名: N-[3-(3,5-dimethyl-phenyl)-1,8-dioxa-2,4-diaza-spiro[4.5]dec-2-en-4-yl]-3-methoxy-2-methyl-benzamide；N-[3-(3,5-dimethyl-phenyl)-1,8-dioxa-2,4-diaza-spiro[4,5]dec-2-en-4-yl]-3-methoxy-2-methyl-benzamide；N-[3-(3,5-dimethylphenyl)-1,8-dioxa-2,4-diazaspiro[4.5]dec-2-en-4-yl]-3-methoxy-2-methylbenzamide
• CAS: 748155-63-7
• 化学式: C₂₃H₂₇N₃O₄
• 分子量: 409.485
• InChiKey: UFEGIGJRTWCKNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.1
• 重原子数：
  30
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  72.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  2-甲基-3-甲氧基苯甲酰氯 在 溶剂黄146 potassium carbonate 、 肼 作用下， 以 甲醇 、 乙醚 、 二氯甲烷 、 氯仿 、 水 为溶剂， 反应 2.67h， 生成 RG-120086
  参考文献：
  名称：

  Oxadiazoline ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

  摘要：

  本发明涉及非甾体配体，用于核受体基于可诱导基因表达系统的使用，以及一种调节外源基因表达的方法，其中包括一个雌激素受体复合物：一个DNA结合结构域；一个配体结合结构域；一个转录激活结构域；和一个配体，与包括外源基因和响应元件的DNA构建物接触；其中外源基因受响应元件控制，DNA结合结构域与响应元件在配体存在的情况下结合导致基因的激活或抑制。

  公开号：

  US20040171651A1

文献信息

• OXADIAZOLINE LIGANDS FOR MODULATING THE EXPRESSION OF EXOGENOUS GENES VIA AN ECDYSONE RECEPTOR COMPLEX
  申请人：Hormann Robert Eugene

  公开号：US20080255210A1

  公开（公告）日：2008-10-16

  The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

  本发明涉及非类固醇配体用于核受体诱导基因表达系统，并提供一种调节外源基因表达的方法，其中包括一个含有雌激素类固醇受体复合物的DNA结合域、配体结合域、转录激活域和配体的接触，与包含外源基因和响应元件的DNA构建物接触；其中，外源基因受响应元件控制，并在配体存在时DNA结合域与响应元件结合导致基因的激活或抑制。
• FUSED CYCLIC MODULATORS OF NUCLEAR HORMONE RECEPTOR FUNCTION
  申请人：Bristol-Myers Squibb Company

  公开号：EP1463728B1

  公开（公告）日：2009-01-14
• EP1601354A4
  申请人：——

  公开号：EP1601354A4

  公开（公告）日：2009-08-12
• Modified Forms of Pseudomonas Exotoxin A
  申请人：JONES Timothy David

  公开号：US20130121983A1

  公开（公告）日：2013-05-16

  Pseudomonas exotoxin A or “PE” is a 66 kD, highly potent, cytotoxic protein secreted by the bacterium Pseudomonas aeruginosa . Various forms of PE have been coupled to other proteins, such as antibodies, to generate therapeutically useful cytotoxin conjugates that selectively target cells of a desired phenotype (such as tumor cells). In the present invention, peptides spanning the sequence of an approximately 38 kD form of Pseudomonas exotoxin A protein were analyzed for the presence of immunogenic CD4+ T cell epitopes. Six immunogenic T cell epitopes were identified. Residues were identified within each epitope for introduction of targeted amino acid substitutions to reduce or prevent immunogenic T-cell responses in PE molecules which may be administered to a heterologous host.
• MODIFIED FORMS OF PSEUDOMONAS EXOTOXIN A
  申请人：INTREXON CORPORATION

  公开号：US20150291941A1

  公开（公告）日：2015-10-15

  Pseudomonas exotoxin A or “PE” is a 66 kD, highly potent, cytotoxic protein secreted by the bacterium Pseudomonas aeruginosa . Various forms of PE have been coupled to other proteins, such as antibodies, to generate therapeutically useful cytotoxin conjugates that selectively target cells of a desired phenotype (such as tumor cells). In the present invention, peptides spanning the sequence of an approximately 38 kD form of Pseudomonas exotoxin A protein were analyzed for the presence of immunogenic CD4+ T cell epitopes. Six immunogenic T cell epitopes were identified. Residues were identified within each epitope for introduction of targeted amino acid substitutions to reduce or prevent immunogenic T-cell responses in PE molecules which may be administered to a heterologous host.