Vintafolide | 742092-03-1

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 长春花生物碱
• 英文名称: Vintafolide
• 英文别名: (2S)-2-[[4-[(2-amino-4-oxo-3H-pteridin-6-yl)methylamino]benzoyl]amino]-5-[[(2S)-1-[[(2S)-5-carbamimidamido-1-[[(2S)-3-carboxy-1-[[(2S)-3-carboxy-1-[[(1R)-1-carboxy-2-[2-[[[(1R,9R,10S,11R,12R,19R)-12-ethyl-4-[(13S,15R,17S)-17-ethyl-17-hydroxy-13-methoxycarbonyl-1,11-diazatetracyclo[13.3.1.04,12.05,10]nonadeca-4(12),5,7,9-tetraen-13-yl]-10,11-dihydroxy-5-methoxy-8-methyl-8,16-diazapentacyclo[10.6.1.01,9.02,7.016,19]nonadeca-2,4,6,13-tetraene-10-carbonyl]amino]carbamoyloxy]ethyldisulfanyl]ethyl]amino]-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
• CAS: 742092-03-1
• 化学式: C₈₆H₁₀₉N₂₁O₂₆S₂
• 分子量: 1917.07
• InChiKey: KUZYSQSABONDME-QRLOMCMNSA-N

物化性质

• 密度：
  1?+-.0.1 g/cm3(Predicted)
• 溶解度：
  溶于二甲基亚砜

计算性质

• 辛醇/水分配系数(LogP)：
  -6.7
• 重原子数：
  135
• 可旋转键数：
  44
• 环数：
  12.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  768
• 氢给体数：
  23
• 氢受体数：
  36

反应信息

• 作为产物：
  描述：

  vinblastine pyridinyl disulfide 、 pteroyl-γ-Glu-Asp-Arg-Asp-Asp-Cys 在 碳酸氢钠 作用下， 以 四氢呋喃 、 水 为溶剂， 以70%的产率得到Vintafolide
  参考文献：
  名称：

  WO2007/22493

  摘要：

  公开号：

文献信息

• [EN] IMPROVED PROCESS FOR A FOLATE-TARGETED AGENT<br/>[FR] PROCÉDÉ PERFECTIONNÉ POUR UN AGENT FOLATE-CIBLÉ
  申请人：ENDOCYTE INC

  公开号：WO2011146707A1

  公开（公告）日：2011-11-24

  The invention described herein pertains to an improved process for preparing the folate-targeted conjugate EC 145 and to the conjugate EC 145 prepared using the improved process, as well as to a pharmaceutical composition comprising the conjugate EC 145 prepared using the improved process.

  本发明涉及一种改进的制备叶酸靶向结合物EC 145的过程，以及使用改进的过程制备的结合物EC 145，以及包括使用改进的过程制备的结合物EC 145的药物组合物。
• FOLATE-TARGETED DIAGNOSTICS AND TREATMENT
  申请人：Leamon Christopher Paul

  公开号：US20120128587A1

  公开（公告）日：2012-05-24

  Methods of detecting and assessing functionally active folate receptors on tumors and treatment associated with those tumors are described. Also described are methods of selecting ovarian and lung cancer patients for therapy with a folate-vinca conjugate by identifying functionally active folate receptors on the tumors of the patient. Also described are methods and compositions for treating folate receptor expressing epithelial tumors with a folate-vinca conjugate in combination with doxorubicin such as pegylated liposomal doxorubicin in which the tumors include ovarian, endometrial or non-small cell lung cancer tumors, including platinum-resistant ovarian tumors and platinum sensitive ovarian tumors. Also described are methods of treating platinum-resistant ovarian cancer using a folate-targeted drug, in the absence or presence of selecting the patient by identifying functionally active folate receptors on the tumors of the patient.

  本文描述了检测和评估肿瘤上功能活性叶酸受体的方法以及与该类肿瘤相关的治疗方法。还描述了通过识别患者肿瘤上功能活性叶酸受体，选择卵巢和肺癌患者使用叶酸-长春瑞滨偶联物疗法的方法。此外，还描述了使用叶酸-长春瑞滨偶联物和多柔比星（如聚乙二醇化脂质体多柔比星）联合治疗表达叶酸受体的上皮性肿瘤的方法和组合物，其中包括卵巢、子宫内膜和非小细胞肺癌肿瘤，包括铂类耐药性卵巢肿瘤和铂类敏感性卵巢肿瘤。此外，还描述了使用叶酸靶向药物治疗铂类耐药性卵巢癌的方法，无论是否通过识别患者肿瘤上功能活性叶酸受体进行患者选择。
• 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.