c-di(2’FdGMP) | 1334145-18-4

• 分子结构分类: 有机化合物 - 核苷、核苷酸和类似物
• 英文名称: c-di(2’FdGMP)
• 英文别名: 2-azanyl-9-[(1~{R},6~{R},8~{R},9~{R},10~{R},15~{R},17~{R},18~{R})-17-(2-azanyl-6-oxidanylidene-1~{H}-purin-9-yl)-9,18-bis(fluoranyl)-3,12-bis(oxidanyl)-3,12-bis(oxidanylidene)-2,4,7,11,13,16-hexaoxa-3$l^{5},12$l^{5}-diphosphatricyclo[13.3.0.0^{6,10}]octadecan-8-yl]-1~{H}-purin-6-one；2-amino-9-[(1R,6R,8R,9R,10R,15R,17R,18R)-17-(2-amino-6-oxo-1H-purin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-dioxo-2,4,7,11,13,16-hexaoxa-3λ5,12λ5-diphosphatricyclo[13.3.0.06,10]octadecan-8-yl]-1H-purin-6-one
• CAS: 1334145-18-4
• 化学式: C₂₀H₂₂F₂N₁₀O₁₂P₂
• 分子量: 694.399
• InChiKey: RKBIDRCIXOIYKC-MJIGAOGXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -4.7
• 重原子数：
  46
• 可旋转键数：
  2
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  301
• 氢给体数：
  6
• 氢受体数：
  16

反应信息

• 作为产物：
  描述：

  [3’-O-(CE)phosphotriester-N²(iB)-2’-deoxy-2’fluoroguanosine]-(3’,5’)-[3’-O-(CE)phosphodiester-N²(iB)-2’-deoxy-2’-fluorog uanosine] 在 吡啶 、 苯甲基-2-磺酰三硝基三氮唑 、 甲胺 作用下， 以 乙醇 为溶剂， 反应 4.0h， 生成 c-di(2’FdGMP)
  参考文献：
  名称：

  [EN] CYCLIC DINUCLEOTIDES FOR CYTOKINE INDUCTION
  [FR] DINUCLÉOTIDES CYCLIQUES FLUORÉS UTILISABLES EN VUE DE L'INDUCTION DES CYTOKINES

  摘要：

  公开号：

  WO2016096174A8

文献信息

• Compositions and methods for activating “stimulator of interferon gene”—dependent signalling
  申请人：ADURO BIOTECH, INC.

  公开号：US10449211B2

  公开（公告）日：2019-10-22

  The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes), In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce human STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are 2′-fluoro substituted, bis-3′,5′CDNs, and most preferably one or more 2′,2″-diF-Rp,Rp, bis-3′,5′CDNs.

  本发明提供了高活性环状二核苷酸（CDN）免疫刺激剂，它能通过最近发现的一种称为 STING（干扰素基因刺激器）的细胞质受体激活直流细胞、本发明的 CDN 以包含一种或多种环状嘌呤二核苷酸的组合物的形式提供，该组合物能诱导人类 STING 依赖性 I 型干扰素的产生、其中组合物中的环嘌呤二核苷酸是2′-氟取代的双-3′,5′CDN，最优选的是一种或多种2′,2″-diF-Rp,Rp,双-3′,5′CDN。
• Compositions and methods for activating “stimulator of interferon gene”13 dependent signalling
  申请人：CHINOOK THERAPEUTICS, INC.

  公开号：US11040053B2

  公开（公告）日：2021-06-22

  The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce human STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are 2′-fluoro substituted, bis-3′,5′ CDNs, and most preferably one or more 2′,2″-diF-Rp,Rp, bis-3′,5′CDNs.

  本发明提供了高活性环状二核苷酸（CDN）免疫刺激剂，可通过最近发现的一种称为 STING（干扰素基因刺激器）的细胞质受体激活 DC。特别是，本发明的 CDN 以组合物的形式提供，该组合物包含一种或多种环状嘌呤二核苷酸，可诱导人类 STING 依赖性 I 型干扰素的产生、其中组合物中的环状嘌呤二核苷酸是 2′-氟取代的双-3′,5′CDN，最优选的是一种或多种 2′,2″-diF-Rp,Rp，双-3′,5′CDN。
• COMPOSITIONS AND METHODS FOR ACTIVATING "STIMULATOR OF INTERFERON GENE" - DEPENDENT SIGNALLING
  申请人：ADURO BIOTECH, INC.

  公开号：US20180064745A1

  公开（公告）日：2018-03-08

  The present invention provides highly active cyclic-di-nucleotide (CDN) immune stimulators that activate DCs via a recently discovered cytoplasmic receptor known as STING (Stimulator of Interferon Genes), In particular, the CDNs of the present invention are provided in the form of a composition comprising one or more cyclic purine dinucleotides induce human STING-dependent type I interferon production, wherein the cyclic purine dinucleotides present in the composition are 2′-fluoro substituted, bis-3′,5′CDNs, and most preferably one or more 2′,2″-diF-Rp,Rp, bis-3′,5′CDNs.
• DC-SIGN ANTIBODY CONJUGATES COMPRISING STING AGONISTS
  申请人：NOVARTIS AG

  公开号：US20210170043A1

  公开（公告）日：2021-06-10

  Provided herein are immunoconjugates comprising an anti-DC-SIGN antibody conjugated to a STING agonist. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.