N-({1-[(4-氯苯基)氨基]-1-氧代-2-丙基}氧基)-3,5-二(三氟甲基)苯甲酰胺 | 285986-88-1

• 物质功能分类: 生物化工 - 抑制剂 - 细胞周期(Cell Cycle)
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: N-({1-[(4-氯苯基)氨基]-1-氧代-2-丙基}氧基)-3,5-二(三氟甲基)苯甲酰胺
• 中文别名: RHOA/C介导基因转录抑制剂(CCG-1423)；N-[2-[(4-氯苯基)氨基]-1-甲基-2-氧乙氧基]-3,5-双(三氟甲基)苯甲酰胺；CCG-1423抑制剂；N-[2-[(4-氯苯基)氨基]-1-甲基-2-氧代乙氧基]-3,5-二(三氟甲基)苯甲酰胺；N-((1-((4-氯苯基)氨基)-1-氧代丙烷-2-基)氧基)-3,5-双(三氟甲基)苯甲酰胺
• 英文名称: n-(2-(4-Chloroanilino)-1-methyl-2-oxoethoxy)-3,5-bis(trifluoromethyl)benzamide
• 英文别名: N-[1-(4-chloroanilino)-1-oxopropan-2-yl]oxy-3,5-bis(trifluoromethyl)benzamide
• CAS: 285986-88-1
• 化学式: C₁₈H₁₃ClF₆N₂O₃
• 分子量: 454.7
• InChiKey: DSMXVSGJIDFLKP-UHFFFAOYSA-N

物化性质

• 溶解度：
  DMSO：可溶5mg/mL，澄清（加热）

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  67.4
• 氢给体数：
  2
• 氢受体数：
  9

安全信息

• WGK Germany：
  3
• 包装等级：
  III
• 危险类别：
  4.1
• 危险性防范说明：
  P240,P210,P241,P264,P280,P302+P352,P370+P378,P337+P313,P305+P351+P338,P362+P364,P332+P313
• 危险品运输编号：
  1325
• 危险性描述：
  H315,H319,H228

制备方法与用途

生物活性

CCG-1423 是一种特定的 RhoA 通路抑制剂，能够抑制 SRF 介导的转录。

体外研究

CCG-1423 选择性地抑制由 Rho 路径信号激活的 SRF 介导的转录，并特异性抑制 LPA 刺激下的 DNA 合成。它还选择性地抑制 RhoC 过表达的黑色素瘤细胞（A375M2 和 SK-Mel-147）的增殖，强烈抑制 PC-3 细胞依赖 Rho 的侵袭。CCG-1423 与 LY294002 结合使用时，能够通过 BMP7 阳性细胞增强小鼠胚胎干细胞向中间中胚层分化。在 H9c2 细胞中，CCG-1423 抑制 MRTF 核定位，并完全阻断 STARS 近端报告基因活性。作为 Rho/MRTF/SRF 通路抑制剂，CCG-1423 还能抑制人结肠成纤维细胞在基质硬度和 TGF-β 刺激下的纤维化过程。

文献信息

• CELL AGGREGATION PROMOTING AGENT
  申请人：Kaneka Corporation

  公开号：EP3733837A1

  公开（公告）日：2020-11-04

  The present invention is directed to providing a means for appropriately controlling the size of cell aggregates without relying on mechanical/physical means. Specifically, the present invention relates to a cell aggregation promoter for use in suspension culture of cells, comprising an SRF inhibitor. The present invention also relates to a method for producing cell aggregates, comprising a step of culturing cells in suspension in a culture medium comprising an SRF inhibitor.

  本发明旨在提供一种不依赖机械/物理手段而适当控制细胞聚集体大小的方法。具体地说，本发明涉及一种用于细胞悬浮培养的细胞聚集促进剂，包括一种 SRF 抑制剂。本发明还涉及一种生产细胞聚集体的方法，包括在含有 SRF 抑制剂的培养基中培养悬浮细胞的步骤。
• Patient treatment via teratogenic pharmaceutical compounds
  申请人：Nant Holdings IP, LLC

  公开号：US11000536B2

  公开（公告）日：2021-05-11

  Compositions and methods for treatment of a condition associated with disease stem cells, and especially cancer stem cells are disclosed. In one aspect, a patient is treated with a stem cell differentiating agent and/or teratogenic pharmaceutical compound to induce one or more destructive pathways in the disease stem cells. Most typically, the destructive pathways include apoptotic pathways, necrotic pathways, and autophagy pathways.

  本文公开了治疗与疾病干细胞，特别是癌症干细胞相关的疾病的组合物和方法。在一个方面，用干细胞分化剂和/或致畸药物化合物治疗患者，以诱导疾病干细胞中的一种或多种破坏途径。最典型的破坏途径包括凋亡途径、坏死途径和自噬途径。
• INHALED STATINS AS BRONCHODILATORS TO IMPROVE LUNG FUNCTION IN RESPIRATORY DISEASES
  申请人：The Regents of the University of California

  公开号：EP3946268A1

  公开（公告）日：2022-02-09
• Methods and Compositions for Modulating RHO-Mediated Gene Transcription
  申请人：Neubig Richard

  公开号：US20090264533A1

  公开（公告）日：2009-10-22

  The present invention is directed to methods and compositions methods and compositions for determining and inhibiting gene transcription in mammalian cells. The invention relates to novel inhibitors of rho-mediated gene transcription and to compounds that may be used as therapeutic agents.
• INHIBITION OF RHO AND OR ROCK AND CELL TRANSPLANTATION
  申请人：BIOAXONE BIOSCIENCES INC.

  公开号：US20150297643A1

  公开（公告）日：2015-10-22

  The present disclosure provides a multi-treatment combination to improve recovery after spinal cord injury or neurotrauma comprising: (a) Cell transplantation at the site of spinal cord injury and (b) Surgical delivery of BA-210. The combined treatment allows cells to be transplanted in the injury site during the acute trauma period, a time when the inflammatory response to neurotrauma adversely effects survival of transplanted cells. Early therapy delivered during critical care treatment after neurotrauma is essential for successful restorative therapy. The multi-treatment combination also provides a method to ensure that multi-potent transplanted cells do not become tumorigenic.