PDK1/Akt/FltDualPathway抑制剂 | 331253-86-2

• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: PDK1/Akt/FltDualPathway抑制剂
• 英文名称: PDK1/Akt/Flt Dual Pathway Inhibitor
• 英文别名: 10,11,12,13,14,16-hexazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(16),2,4,6,9,12,14-heptaen-8-one
• CAS: 331253-86-2
• 化学式: C₁₀H₄N₆O
• 分子量: 224.181
• InChiKey: DPANHMGWPXVBQI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.7
• 重原子数：
  17
• 可旋转键数：
  0
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  85.9
• 氢给体数：
  0
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  6-马来酰亚胺己酸肼 、 蛋白激酶B抑制剂/AKT抑制剂 、 PDK1/Akt/FltDualPathway抑制剂 在 吡啶 作用下， 生成 、
  参考文献：
  名称：

  一种水溶性KP372-1衍生物及其制备方法

  摘要：

  本发明公开一种KP372‑1衍生物及其制备方法，利用了马来酰胺官能团和巯基官能团实现KP372‑1与水溶性氨基酸的嵌合；通过化学修饰进行衍生物的制备，反应整体收率较高，过程中使用的试剂较为常见易得，且合成过程中步骤简单，操作容易，可以广泛应用于工业生产，为后期KP372‑1的临床应用奠定了物质基础。

  公开号：

  CN112457315A
• 作为产物：
  描述：

  四唑-1,5-二胺 、 水合茚三酮 生成 蛋白激酶B抑制剂/AKT抑制剂 、 PDK1/Akt/FltDualPathway抑制剂
  参考文献：
  名称：

  Tetracyclic inhibitors of cysteine proteases, the pharmaceutical compositions thereof and their therapeutic applications

  摘要：

  本发明涉及公式（I）的新化合物，它们的制备过程以及它们的治疗用途，其中R3、R4、R5、R6、Y、Het1、T、U、V、W、X、Ru、Rv和Rw如权利要求1所定义。

  公开号：

  EP1918292A1

文献信息

• FUSED THIOPHENES AS DUAL INHIBITORS OF EGFR/VEGFR AND THEIR USE IN THE TREATMENT OF CANCER
  申请人：Deng Huayun

  公开号：US20120295965A1

  公开（公告）日：2012-11-22

  Disclosed are compositions and methods related to identification of modulators of EGFR and VEGFR.

  本发明涉及识别EGFR和VEGFR的调节剂的组合物和方法。
• METHODS AND COMPOSITIONS FOR MALIC ENZYME 2 (ME2) AS A TARGET FOR CANCER THERAPY
  申请人：Sukhatme Vikas P.

  公开号：US20130209488A1

  公开（公告）日：2013-08-15

  The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing cancer and other related diseases that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include combination therapy, such as with a combination of two or more ME2 inhibitors or a combination of an ME2 inhibitor and an anticancer agent.
• IGF1 BIOMARKER FOR IGF1R INHIBITOR THERAPY
  申请人：MERCK SHARP & DOHME CORP.

  公开号：US20150056191A1

  公开（公告）日：2015-02-26

  The present invention provides, inter alia, methods for treating tumors that are sensitive to an IGF1R inhibitor. The tumor are determined to be sensitive if the level of IGF1 mRNA expression in the tumor cells, relative to one or more reference genes, reaches a certain threshold level. Methods for evaluating patients as candidates for receipt of the IGF1R inhibitor therapy are also provided as well along with in vitro assay methods and kits for performing any of the methods.
• METHODS OF TREATING PROLIFERATIVE DISORDERS WITH MALATE OR DERIVATIVES THEREOF
  申请人：Sukhatme Vikas P.

  公开号：US20150056215A1

  公开（公告）日：2015-02-26

  The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing proliferative disorders, such as cancel-, that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include monotherapy with malate, or a derivative thereof, as well as combination therapy, such as malate, or a derivative thereof, combined with another therapeutic agent, such as a malic enzyme 2 inhibitor, an antineoplastic agent, a glycolysis inhibitor, an antiangiogenic agent, an immunomodulatory agent, an antibody, or a cytokine.
• KP372-1-INDUCED DNA DAMAGE AS A CHEMOTHERAPEUTIC APPROACH TO TREAT CANCER
  申请人：New Mexico Tech University Research Park Corporation

  公开号：US20220143033A1

  公开（公告）日：2022-05-12

  Disclosed herein are methods of treating a cancer that overexpresses NQO1 comprising administering KP372-1. In some embodiments, KP372-1 is administered with a polymerase inhibitor.