WP 1034 | 857064-42-7

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: WP 1034
• 英文别名: (E)-2-cyano-3-(4-nitrophenyl)-N-[(1R)-1-phenylethyl]prop-2-enamide
• CAS: 857064-42-7
• 化学式: C₁₈H₁₅N₃O₃
• 分子量: 321.335
• InChiKey: RYYNDHCHTCVQJH-KWWJGWKXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  24
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  98.7
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• TRYPHOSTIN-ANALOGS FOR THE TREATMENT OF CELL PROLIFERATIVE DISEASES
  申请人：Donato Nicholas J

  公开号：US20100292229A1

  公开（公告）日：2010-11-18

  The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. In general aspects, compounds of the present invention are tyrphostin-like in structure. Compounds of the present invention, in certain embodiments, display significant potency by causing, for example, inhibition of Stat3 activation, reduction in c-myc protein levels and/or induction of apoptosis in tumor cells. In general aspects, compounds of the present invention induce one or more of these activities at nanomolar concentrations and typically function through a unique mechanism involving the induction of stress granules that bind specific signaling molecules and prevent them from participating in signal transduction and oncogenesis.

  本发明涉及化合物及其用于治疗细胞增殖性疾病，如癌症。在一般方面，本发明的化合物在结构上类似于酪氨酸激酶抑制剂。在某些实施例中，本发明的化合物通过诱导应激颗粒结合特定信号分子并阻止它们参与信号转导和肿瘤发生，从而表现出显著的效力，例如抑制Stat3激活、降低c-myc蛋白水平和/或诱导肿瘤细胞凋亡。在一般方面，本发明的化合物在纳摩尔浓度下诱导这些活性中的一个或多个，并通常通过诱导应激颗粒的独特机制发挥作用，这些应激颗粒结合特定信号分子并防止它们参与信号转导和肿瘤发生。
• Compounds for treatment of cell proliferative diseases
  申请人：BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM

  公开号：EP2487156A1

  公开（公告）日：2012-08-15

  The present invention concerns compounds and their use to treat cell proliferative diseases such as cancer. Compounds of the present invention display significant potency as kinase inhibitors, cause the downregulation of c-myc, and inhibit the growth and survival of cancerous cell lines.

  本发明涉及化合物及其用于治疗癌症等细胞增殖性疾病。本发明的化合物作为激酶抑制剂具有显著的效力，可导致 c-myc 下调，抑制癌细胞株的生长和存活。
• Natural-killer/T-cell lymphoma (NKTCL) susceptibility prediction, diagnosis and therapy
  申请人：SINGAPORE HEALTH SERVICES PTE LTD

  公开号：US10378062B2

  公开（公告）日：2019-08-13

  Natural-KilleifT-Cell Lymphoma (NKTCL) susceptibility prediction, diagnosis and therapy. The invention relates to a method for predicting Natural Killer T-cell Lymphoma (NKTCL) susceptibility and/or diagnosing NKTCL in a subject comprising testing for JAK mutations. The invention also relates to a method of screening for candidate agents capable of treating NKTCL using a cell line comprising at least one JAK mutation. The invention includes an NKTCL animal model comprising at least one JAK mutation. The invention also includes JAK inhibitors for treating NKTCL.

  天然杀伤T细胞淋巴瘤（NKTCL）易感性预测、诊断和治疗。本发明涉及一种预测天然杀伤T细胞淋巴瘤（NKTCL）易感性和/或诊断受试者NKTCL的方法，包括检测JAK突变。本发明还涉及一种利用包含至少一种 JAK 突变的细胞系筛选能够治疗 NKTCL 的候选药物的方法。本发明包括一种包含至少一种 JAK 突变的 NKTCL 动物模型。本发明还包括用于治疗NKTCL的JAK抑制剂。
• INTERFERON THERAPIES IN COMBINATION WITH BLOCKADE OF STAT3 ACTIVATION
  申请人：Board of Regents, The University of Texas System

  公开号：EP2506852A2

  公开（公告）日：2012-10-10
• EP2782562A2
  申请人：——

  公开号：EP2782562A2

  公开（公告）日：2014-10-01