GW2974 | 202272-68-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶并嘧啶类
• 英文名称: GW2974
• 英文别名: N⁴-(1-benzyl-1H-indazol-5-yl)-N⁶,N⁶-dimethyl-pyrido-[3,4-d]-pyrimidine-4,6-diamine；GW 2974；4-N-(1-benzyl-1H-indazol-5-yl)-6-N,6-N-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine；N4-(1-benzyl-1H-indazol-5-yl)-N6,N6-dimethyl-pyrido[3,4-d]pyrimidine-4,6-diamine；N6,N6-dimethyl-N4-[1-(phenylmethyl)-5-indazolyl]pyrido[3,4-d]pyrimidine-4,6-diamine；4-N-(1-benzylindazol-5-yl)-6-N,6-N-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine
• CAS: 202272-68-2
• 化学式: C₂₃H₂₁N₇
• 分子量: 395.467
• InChiKey: DYYZXRCFCVDSKD-UHFFFAOYSA-N

物化性质

• 溶解度：
  二甲基亚砜：≥20mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  30
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  71.8
• 氢给体数：
  1
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  4,6-二氯吡啶[3,4-D]并嘧啶 以 乙醇 、 乙腈 为溶剂， 生成 GW2974
  参考文献：
  名称：

  Indazolylamino quinazolines and pyridopyrimidines as inhibitors of the EGFr and c-erbB-2

  摘要：

  Described herein is the design and synthesis of indazolylaminopyridopyrimidines and quinazolines as inhibitors of the class 1 tyrosine kinase receptor family. Data is presented for N-4-(1-benzyl-1H-indazol-5-yl)-N-6,N-6-dimethylpyrido[3,4-d]pyrimidine-4,6-diamine 3B. This compound inhibited EGFr and c-erbB-2 enzymes selectively over other kinases. It inhibited the proliferation of a range of tumour cell lines in vitro and the growth of BT474 xenografts in SCID mice. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(01)00219-0

文献信息

• [EN] CANCER TREATMENT METHOD<br/>[FR] METHODE DE TRAITEMENT DU CANCER
  申请人：SMITHKLINE BEECHAM CORP

  公开号：WO2005046678A1

  公开（公告）日：2005-05-26

  The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and a PI3K and/or Akt inhibitor to a mammal suffering from a cancer.

  本发明涉及一种治疗哺乳动物癌症的方法以及在这种治疗中有用的药物组合。具体而言，该方法涉及一种癌症治疗方法，其中向患有癌症的哺乳动物施用一种erb家族抑制剂和一种PI3K和/或Akt抑制剂。
• Cancer treatment method comprising administering an erb-family inhibitor and a raf and/or ras inhibitor
  申请人：Spector Lee Neil

  公开号：US20050176740A1

  公开（公告）日：2005-08-11

  The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and a Raf and/or ras inhibitor to a mammal suffering from a cancer.

  本发明涉及一种治疗哺乳动物癌症的方法和在这种治疗中有用的药物组合。具体来说，该方法涉及一种癌症治疗方法，包括向患有癌症的哺乳动物施用erb家族抑制剂和Raf和/或ras抑制剂。
• Cancer treatment method
  申请人：Dev Kumar Inderjit

  公开号：US20070161665A1

  公开（公告）日：2007-07-12

  The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering an erb family inhibitor and a PI3K and/or Akt inhibitor to a mammal suffering from cancer.

  本发明涉及一种治疗哺乳动物癌症的方法，以及在这种治疗中有用的药物组合。具体而言，该方法涉及一种癌症治疗方法，包括向患有癌症的哺乳动物施用erb家族抑制剂和PI3K和/或Akt抑制剂。
• METHOD FOR DETERMINING SENSITIVITY OF TUMOR CELLS TO TYROSINE KINASE INHIBITOR AND COMPUTER PROGRAM PRODUCT
  申请人：KAWAI Masaaki

  公开号：US20110318768A1

  公开（公告）日：2011-12-29

  The present invention provides a method for determining sensitivity of the tumor cells to an EGFR and/or HER 2 inhibitor by evaluating inhibitory capacity of an Src inhibitor in a sample for measuring tyrosine kinase activity which is prepared from a biological sample containing tumor cells, a computer program and a method for determining effectiveness.

  本发明提供了一种方法，通过评估样本中Src抑制剂的抑制能力，测量来自含有肿瘤细胞的生物样本的酪氨酸激酶活性，以确定肿瘤细胞对EGFR和/或HER2抑制剂的敏感性，以及一种用于确定有效性的计算机程序和方法。
• Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
  申请人：GLAXO GROUP LIMITED

  公开号：EP1304110A2

  公开（公告）日：2003-04-23

  Protein tyrosine kinase inhibitor compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds, and their use in medicine, for example in the treatment of cancer and psoriasis. In particular, the use of an inhibitor of both EGFR and erbB-2 in the treatment of a susceptible malignancy, such as cancer or a malignant tumour, is described.

  本文描述了蛋白酪氨酸激酶抑制剂化合物、其制备方法、包括此类化合物的药物组合物及其在医学中的用途，例如在治疗癌症和牛皮癣中的用途。特别介绍了表皮生长因子受体和erbB-2抑制剂在治疗易感恶性肿瘤（如癌症或恶性肿瘤）中的应用。