Fmoc-Ala-PAB-Br | 1192581-24-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: Fmoc-Ala-PAB-Br
• CAS: 1192581-24-0
• 化学式: C₂₅H₂₃BrN₂O₃
• 分子量: 479.373
• InChiKey: ZTGAQOBOOTUMTH-INIZCTEOSA-N

物化性质

• 沸点：
  688.5±50.0 °C(predicted)
• 密度：
  1.415±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.45
• 重原子数：
  31.0
• 可旋转键数：
  6.0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  67.43
• 氢给体数：
  2.0
• 氢受体数：
  3.0

反应信息

• 作为反应物：
  描述：

  Fmoc-Ala-PAB-Br 、 3-O-methylfluorescein 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以45 mg的产率得到
  参考文献：
  名称：

  CN114835722

  摘要：

  公开号：
• 作为产物：
  描述：

  Fmoc-L-丙氨酸 在 三溴化磷 、 2-乙氧基-1-乙氧碳酰基-1,2-二氢喹啉 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 36.0h， 生成 Fmoc-Ala-PAB-Br
  参考文献：
  名称：

  膀胱癌近红外荧光成像的可肾脏清除的大分子报告基因。

  摘要：

  膀胱癌（BC）是一种高发病率和高死亡率的流行疾病。然而，由于缺乏具有高肾清除率的癌症特异性光学剂，因此对BC进行体内光学成像仍然具有挑战性。本文中，合成了一个大分子报告基因（CyP1），用于在活小鼠中进行BC的实时近红外荧光（NIRF）成像和尿液分析。由于高的肾脏清除率（注射后24 h约占注射剂量的94％）及其癌症生物标志物（APN =氨基肽酶N）的特异性，CyP1可以有效地转运至膀胱，并特别开启其NIRF信号至报告检测活小鼠中的BC。此外，CyP1可用于光学尿液分析，允许离体追踪肿瘤进展以进行治疗评估，并易于翻译CyP2作为体外诊断测定法。

  DOI：

  10.1002/anie.201911859

文献信息

• Multiplex Optical Urinalysis for Early Detection of Drug-Induced Kidney Injury
  作者：Penghui Cheng、Qingqing Miao、Jiaguo Huang、Jingchao Li、Kanyi Pu

  DOI：10.1021/acs.analchem.0c00989

  日期：2020.4.21

  Drug-induced kidney injury (DIKI) is a significant contributor of both acute and chronic kidney injury and remains a major concern in drug development and clinical care. However, current clinical diagnostic methods often fail to accurately and timely detect nephrotoxicity. This study reports the development of activatable molecular urinary reporters (MURs) that are able to specifically detect urinary biomarkers including γ-glutamyl transferase (GGT), alanine aminopeptidase (AAP), and N-acetyl-β-d-glucosaminidase (NAG). By virtue of their discrete absorption and emission properties, the mixture of MURs can serve as a cocktail sensor for multiplex optical urinalysis in the mouse models of drug-induced acute kidney injury (AKI) and chronic kidney disease (CKD). The MURs cocktail not only detects nephrotoxicity earlier than the tested clinical diagnostic methods in drug-induced AKI and CKD mice models, but also possesses a higher diagnostic accuracy. Therefore, MURs hold great promise for detection of kidney function in both preclinical drug screening and clinical settings.

  这项研究报告了一种可激活的分子尿液报告分子(MURs)的开发,这些分子能够特异性检测包括γ-谷氨酰转移酶(GGT)、丙氨酸氨基肽酶(AAP)和N-乙酰-β-D-氨基葡萄糖苷酶(NAG)在内的尿液生物标志物。由于它们具有独特的吸收和发射特性,MURs混合物可以作为多重光学尿液分析的鸡尾酒传感器,用于药物诱导的急性肾损伤(AKI)和慢性肾病(CKD)的小鼠模型研究。 在药物诱导的AKI和CKD小鼠模型中,MURs鸡尾酒不仅能比现有的临床诊断方法更早地检测到肾毒性,而且具有更高的诊断准确性。因此,MURs在临床前药物筛选和临床应用中对肾功能的检测具有广阔的应用前景。
• Novel immunoconjugates comprised of streptonigrin and 17-amino-geldanamycin attached via a dipeptide-p-aminobenzyl-amine linker system
  作者：Patrick J. Burke、Brian E. Toki、David W. Meyer、Jamie B. Miyamoto、Kim M. Kissler、Martha Anderson、Peter D. Senter、Scott C. Jeffrey

  DOI：10.1016/j.bmcl.2009.03.145

  日期：2009.5

  Cytotoxic agents streptonigrin and 17-amino-geldanamycin were linked to monoclonal antibodies (mAbs), forming antibody-drug conjugates (ADCs) for antigen-mediated targeting to cancer cells. The drugs were conjugated with a linker construct that is labile to lysosomal proteases and incorporates a valine-alanine-p-aminobenzyl (PAB)-amino linkage for direct attachment to the electron-deficient amine functional groups present in both drugs. The resulting ADCs release drug following internalization into antigen-positive cancer cells. The drug linkers were conjugated to mAbs cAC10 (anti-CD30) and h1F6 (anti-CD70) via alkylation of reduced interchain disulfides to give ADCs loaded with 4 drugs/mAb. The streptonigrin ADCs were potent and immunologically specific on a panel of cancer cell lines in vitro and in a Hodgkin lymphoma xenograft model. We conclude that streptonigrin ADCs are candidates for further research, and that the novel linker system used to make them is well-suited for the conjugation of cytotoxic agents containing electron-deficient amine functional groups. (C) 2009 Elsevier Ltd. All rights reserved.
• CN116621819
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  公开号：——

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