cabazitaxel-2′-succinyl | 1375468-12-4

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: cabazitaxel-2′-succinyl
• 英文别名: 4-[(2R,3S)-1-[[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-2-benzoyloxy-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-15-yl]oxy]-3-[(2-methylpropan-2-yl)oxycarbonylamino]-1-oxo-3-phenylpropan-2-yl]oxy-4-oxobutanoic acid
• CAS: 1375468-12-4
• 化学式: C₄₉H₆₁NO₁₇
• 分子量: 936.02
• InChiKey: IKUPVMXMSHZTTI-XVKOHUKFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  67
• 可旋转键数：
  20
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  246
• 氢给体数：
  3
• 氢受体数：
  17

反应信息

• 作为反应物：
  描述：

  cabazitaxel-2′-succinyl 、 bis(prop-2-enyl) (2S)-2-[[(2S)-6-amino-1-oxo-1-prop-2-enoxyhexan-2-yl]carbamoylamino]pentanedioate 在 N,N'-二环己基碳二亚胺 、 吗啉 、 四(三苯基膦)钯 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 PSMA-cabazitaxel
  参考文献：
  名称：

  [EN] TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
  [FR] CONJUGUÉS CIBLÉS, PARTICULES ET PRÉPARATIONS ASSOCIÉES

  摘要：

  包括纳米颗粒和微粒子在内的粒子以及其制剂，包括将活性药剂（如治疗、预防或诊断药剂）与靶向基团通过连接剂结合的共轭物。这些设计可以提供改善活性药剂的时间空间传递和/或改善生物分布的效果。提供了制备共轭物、粒子和制剂的方法。提供了向需要的受试者（例如治疗或预防癌症或传染病）施用制剂的方法。

  公开号：

  WO2016004043A1
• 作为产物：
  描述：

  丁二酸酐 、 卡巴他赛 在 吡啶 、 potassium hydroxide 作用下， 以80%的产率得到cabazitaxel-2′-succinyl
  参考文献：
  名称：

  Polymeric conjugates of active principles, their process of preparation and their polymeric intermediates

  摘要：

  本发明涉及将活性成分接枝到聚合物的新型共轭物，以及包括它们的纳米粒子，它们的制备和它们的聚合物中间体。

  公开号：

  US09278137B2

文献信息

• 一种抗肿瘤药物偶联物、制备方法、制剂和应 用
  申请人：浙江大学

  公开号：CN106317067B

  公开（公告）日：2018-04-17

  本发明公开了一种抗肿瘤药物偶联物、制备方法及其纳米胶束制备和应用。本发明提供的偶联物的结构式如式(I)所示，由7‑乙基‑10‑羟基喜树碱和紫杉醇类抗肿瘤药物通过连接键连接而成，其中，L为连接键；R1为苯基或叔丁氧基，R2为乙酰基、H或甲基，R3为H或甲基，步骤简单，制备成本低，稳定性高，安全性好，符合临床用药的要求，适用于大规模工业化生产。本发明还公开如式(I)所示抗肿瘤药物偶联与两亲性聚合物组成的纳米胶束及其抗肿瘤的应用，体内试验显示纳米胶束良好的抗肿瘤效果，具有较好的市场前景与价值。
• Targeted Conjugates Encapsulated in Particles and Formulations Thereof
  申请人：Blend Therapeutics, Inc.

  公开号：US20140187501A1

  公开（公告）日：2014-07-03

  Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, containing conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.

  包括纳米颗粒和微粒在内的微粒子以及其药物配方，其中含有活性剂的共轭物，例如治疗、预防或诊断剂，通过连接体连接到靶向基团，已经设计出来，可以提供改善活性剂的时间空间传递和/或改善生物分布的效果。提供了制备共轭物、微粒子和其配方的方法。提供了将这些配方用于需要的受试者的方法，例如用于治疗或预防癌症或传染病。
• Coupling the near-infrared fluorescent dye IR-780 with cabazitaxel makes renal cell carcinoma chemotherapy possible
  作者：Yu Zheng、Ting Lan、Di Wei、Geng Zhang、Guangdong Hou、Jiarui Yuan、Fei Yan、Fuli Wang、Ping Meng、Xiaojian Yang、Guo Chen、Zheng Zhu、Zifan Lu、Wei He、Jianlin Yuan

  DOI：10.1016/j.biopha.2019.109001

  日期：2019.8

  Renal cell carcinoma (RCC) has always been considered resistant to chemotherapy. IR-780 is a near-infrared fluorescent (NIRF) dye that can be efficiently taken up by RCC cells. Cabazitaxel is a cytotoxic drug that interferes with mitosis by acting on tubulin. We chemically fused IR-780 and cabazitaxel into a new drug, Caba-780, which is expected to increase the sensitivity of RCC to chemotherapy. Infrared spectrum, nuclear magnetic resonance spectra, high-resolution mass spectra, and IR spectra were used for detecting structural characterization of the new synthetic drug Caba-780. The RCC cells lines ACHN and 786-0, as well as the non-cancerous human embryonic kidney cell line HEK293, were used to assess the cytotoxicity and tumor-efficient uptake of Caba-780 in vitro. The xenograft tumor-bearing mice and C57 mice were used to estimate the tumor-efficient imaging of Caba-780 as well as the safety and efficacy of its anti-tumor effects in vivo. The new synthetic drug Caba-780 retains the NIRF properties of IR-780. In vitro, Caba-780 was efficiently absorbed by the RCC cell lines ACHN and 786-0, and had an inhibitory effect on their growth, clonogenicity migration, and invasion. At the same time, Caba-780 retained the anti-tumor effect of cabazitaxel, which can inhibit the growth of tumor cells and promote apoptosis by inhibiting mitosis. In vivo experiments showed that Caba-780 can be taken up and imaged in tumor tissue, whereby it inhibits tumor growth. The novel fused molecule Caba-780 has application prospects in the diagnosis and treatment of RCC and makes RCC chemotherapy possible.
• POLYMERIC CONJUGATES OF ACTIVE PRINCIPLES, THEIR PROCESS OF PREPARATION AND THEIR POLYMERIC INTERMEDIATES
  申请人：Amgoune Abderrhamane

  公开号：US20130243719A1

  公开（公告）日：2013-09-19

  The present invention relates to novel conjugates of active principles grafted to a polymer, to the nanoparticles comprising them, to their preparation and to their polymeric intermediates.
• TARGETED CONJUGATES AND PARTICLES AND FORMULATIONS THEREOF
  申请人：TARVEDA THERAPEUTICS, INC.

  公开号：US20170151339A1

  公开（公告）日：2017-06-01

  Particles, including nanoparticles and microparticles, and pharmaceutical formulations thereof, comprising conjugates of an active agent such as a therapeutic, prophylactic, or diagnostic agent attached to a targeting moiety via a linker have been designed which can provide improved temporospatial delivery of the active agent and/or improved biodistribution. Methods of making the conjugates, the particles, and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer or infectious diseases.