N-乙酰基多柔比星 | 69299-74-7

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 蒽环类药物
• 中文名称: N-乙酰基多柔比星
• 英文名称: N-[3-hydroxy-2-methyl-6-[[(1S,3S)-3,5,12-trihydroxy-3-(2-hydroxyacetyl)-10-methoxy-6,11-dioxo-2,4-dihydro-1H-tetracen-1-yl]oxy]oxan-4-yl]acetamide
• CAS: 69299-74-7
• 化学式: C₂₉H₃₁NO₁₂
• 分子量: 585.6
• InChiKey: WMMDWCWHMHGCSH-JKHBLNKOSA-N

物化性质

• 沸点：
  895.1±65.0 °C(Predicted)
• 密度：
  1.58±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.5
• 重原子数：
  42
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  209
• 氢给体数：
  6
• 氢受体数：
  12

文献信息

• Remote detection of substance delivery to cells
  申请人：Drummond C. Daryl

  公开号：US20050112065A1

  公开（公告）日：2005-05-26

  The present invention provides for the development of endocytosis-sensitive probes, and a remote method for measuring cellular endocytosis. These probes are based on the reduced water permeability of a nanoparticle or liposomal delivery system, and inherent degradability or disruption of barrier integrity upon endocytosis. The invention also provides for liposomes having combined therapeutic and diagnostic utilities by co-encapsulating ionically coupled diagnostic and therapeutic agents, in one embodiment, by a method using anionic chelators to prepare electrochemical gradients for loading of amphipathic therapeutic bases into liposomes already encapsulating an imaging agent. The invention provides for imaging of therapeutic liposomes by inserting a lipopolymer anchored, remotely sensing reporter molecules into liposomal lipid layer. The invention allows for an integrated delivery system capable of imaging molecular fingerprints in diseased tissues, treatment, and treatment monitoring.

  本发明提供了一种用于开发内吞敏感探针的方法，以及一种测量细胞内吞的远程方法。这些探针基于纳米颗粒或脂质体递送系统的降低水透性，以及内吞时固有的可降解性或屏障完整性破坏。该发明还提供了一种具有联合治疗和诊断功能的脂质体，通过共包埋离子耦合的诊断和治疗剂，其中一种实施方式是使用阴离子螯合剂的方法，为脂质体内已包埋成像剂的脂质体加载两性治疗碱。该发明通过将脂质体脂质层插入脂质聚合物锚定的远程感测报告分子来成像治疗脂质体。该发明允许集成递送系统成像疾病组织中的分子指纹，治疗和治疗监测。
• [EN] STABLE DOXORUBICIN/LIPOSOME COMPOSITION
  申请人：LIPOSOME TECHNOLOGY, INC.

  公开号：WO1992002208A1

  公开（公告）日：1992-02-20

  (EN) A lyophilized doxorubicin/lipid composition which is stable against doxorubicin breakdown on storage. The composition is formed by lyophilizing a doxorubicin liposome suspension having a pH between 3.0 and 4.4.(FR) Composition de doxorubicine/lipide lyophilisée ne souffrant pas de la dégradation de la doxorubicine lors du stockage. La composition est formée par lyophilisation d'une suspension de liposomes de doxorubicine ayant un pH compris entre 3,0 et 4,4.

  一种冻干的多柔比星/脂质组合物，其在贮存时稳定不会分解多柔比星。该组合物是通过将pH在3.0至4.4之间的多柔比星脂质体悬浮液冻干形成的。
• Liposomes with enhanced circulation time and method of treatment
  申请人：Alza Corporation

  公开号：US20010051183A1

  公开（公告）日：2001-12-13

  A liposome composition for localizing an anti-tumor compound to a solid tumor via the bloodstream. The liposomes, which contain the agent in entrapped form, are composed of vesicle-forming lipids and between 1-20 mole percent of a vesicle-forming lipid derivatized with hydrophilic biocompatible polymer, and have sizes in a selected size range between 0.07 and 0.12 microns. After intravenous administration, the liposomes are taken up by the tumor within 24-48 hours, for site-specific release of entrapped compound into the tumor. In one composition for use in treating a solid tumor, the compound is an anthracycline antibiotic drug which is entrapped in the liposomes at a concentration of greater than about 50 &mgr;g agent/&mgr;mole liposome lipid. The method results in regression of solid colon and breast carcinomas which are refractory to anthracycline antibiotic drugs administered in free form or entrapped in conventional liposomes.

  一种通过血液定位抗肿瘤化合物到实体肿瘤的脂质体组合物。这些脂质体包含被困在其中的药物，由成泡脂质和1-20摩尔百分比的被水亲和性生物相容性聚合物衍生的成泡脂质组成，并且具有在0.07和0.12微米之间的选择性大小范围。静脉注射后，脂质体在24-48小时内被肿瘤吸收，以便将被困住的化合物定点释放到肿瘤中。在一种用于治疗实体肿瘤的组合物中，该化合物是一种蒽环类抗生素药物，其浓度大于50微克药物/微摩尔脂质体脂质。该方法导致对于自由形式或被困在常规脂质体中的蒽环类抗生素药物无效的实体结肠和乳腺癌的退缩。
• Liposomes useful for drug delivery
  申请人：Hong Keelung

  公开号：US20070116753A1

  公开（公告）日：2007-05-24

  The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provide methods of making the liposome compositions provided by the present invention.

  本发明提供了含有取代铵和/或多阴离子的脂质体组合物，可选地含有所需的治疗或成像实体。本发明还提供了制备本发明所提供的脂质体组合物的方法。
• Liposomes Useful for Drug Delivery
  申请人：Hong Keelung

  公开号：US20120171283A1

  公开（公告）日：2012-07-05

  The present invention provides liposome compositions containing substituted ammonium and/or polyanion, and optionally with a desired therapeutic or imaging entity. The present invention also provides methods of making the liposome compositions provided by the present invention.

  本发明提供了含有取代铵和/或多阴离子的脂质体组合物，可选择性地含有所需的治疗或成像实体。本发明还提供了制备本发明所提供的脂质体组合物的方法。