CGP076030 | 497152-38-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯
• 英文名称: CGP076030
• 英文别名: 7H-Pyrrolo(2,3-d)pyrimidin-4-amine, 7-(4-(2-((2-methoxyethyl)amino)ethoxy)phenyl)-5-(3-methoxyphenyl)-；7-[4-[2-(2-methoxyethylamino)ethoxy]phenyl]-5-(3-methoxyphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
• CAS: 497152-38-2
• 化学式: C₂₄H₂₇N₅O₃
• 分子量: 433.51
• InChiKey: QTVVTRCTOOWLSI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  32
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  96.4
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Combination product of inhibitor of the src family of non-recetpor tyrosine kinases and gemcitabine
  申请人：Barge Alan

  公开号：US20060142297A1

  公开（公告）日：2006-06-29

  The invention concerns a combination comprising an inhibitor of Src kinase and the cytotoxic agent gemcitabine, a pharmaceutical composition comprising such a combination and its use in the treatment or prophylaxis of cancer, particularly of pancreatic cancer.

  本发明涉及一种组合物，包括Src激酶抑制剂和细胞毒素吉西他滨，一种含有该组合物的药物组合物以及其在治疗或预防癌症，特别是胰腺癌方面的用途。
• Therapeutic agents comprising an anti-angiogenic agent in combination with an src-inhibitor and their therapeutic use
  申请人：Curwen Owen Jon

  公开号：US20060223815A1

  公开（公告）日：2006-10-05

  The invention relates to the use of an anti-angiogenic agent in combination with an inhibitor of the Src family of non-receptor tyrosine kinases in the manufacture of a medicament for use in the substantially normotensive treatment in a warm-blooded mammal such as a human being of a disease state associated with angiogenesis, the Src kinase inhibitor being administered in an amount effective to counteract substantially the hypertension induced by the anti-angiogenic agent.

  本发明涉及在制造一种药物时使用抗血管生成剂与Src家族非受体酪氨酸激酶抑制剂相结合，用于治疗与血管生成有关的疾病状态，如在温血哺乳动物（如人类）中进行实质性正常血压治疗。 Src激酶抑制剂的用量有效地对抗抗血管生成剂引起的高血压。
• Multi-Functional Small Molecules as Anti-Proliferative Agents
  申请人：Cai Xiong

  公开号：US20080221132A1

  公开（公告）日：2008-09-11

  The present invention relates to the compositions, methods, and applications of a novel approach to selective inhibition of several cellular or molecular targets with a single small molecule. More specifically, the present invention relates to multi-functional small molecules wherein one functionality is capable of inhibiting histone deacetylases (HDAC) and the other functionality is capable of inhibiting a different cellular or molecular pathway involved in aberrant cell proliferation, differentiation or survival.

  本发明涉及一种新型选择性抑制多种细胞或分子靶点的组合物、方法和应用。更具体地说，本发明涉及多功能小分子，其中一种功能能够抑制组蛋白去乙酰化酶（HDAC），另一种功能能够抑制与异常细胞增殖、分化或存活有关的不同细胞或分子途径。
• THERAPEUTIC AGENTS COMPRISING AN ANTI-ANGIOGENIC AGENT IN COMBINATION WITH AN SRC-INHIBITOR AND THEIR THERAPEUTIC USE
  申请人：CURWEN Jon Owen

  公开号：US20100029673A1

  公开（公告）日：2010-02-04

  The invention relates to a method for the production of an anti-cancer effect or a method for the treatment of a sold tumour disease by administration of an anti-angiogenic agent selected from 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline and 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline and pharmaceutically-acceptable acid-addition salts thereof, in combination with a Src kinase inhibitor selected from 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline and pharmaceutically-acceptable acid-addition salts thereof.

  本发明涉及一种通过给予选择自4-(4-氟-2-甲基吲哚-5-氧基)-6-甲氧基-7-(3-(吡咯烷-1-基)丙氧基)喹唑啉和4-(4-溴-2-氟苯胺基)-6-甲氧基-7-(1-甲基哌啶-4-基甲氧基)喹唑啉及其药学上可接受的酸盐，结合选择自4-(6-氯-2,3-亚甲二氧基苯胺基)-7-[2-(4-甲基哌嗪-1-基)乙氧基]-5-四氢吡喃-4-氧基喹唑啉及其药学上可接受的酸盐的Src激酶抑制剂，以产生抗癌效应或治疗固体肿瘤疾病的方法。
• Prostate cancer cell lines, gene signatures and uses thereof
  申请人：Pestell Richard G.

  公开号：US10952415B2

  公开（公告）日：2021-03-23

  The present disclosure, in part, is directed to a mammalian prostate cancer cell line comprising at least one or a set of primary mammalian epithelial cells which have been infected with a retroviral vector carrying an oncogene selected from the group consisting of c-Myc, Ha-Ras, NeuT, c-Src and combinations thereof and in which said gene is expressed. Applications of the pro-state cell lines, including immune competent animal models of prostate cancer, a method for the in vitro production of immortalized primary mammalian epithelial cells, a method of determining whether a human subject having prostate cancer is suffering from or at risk for developing metastasis, a method of preventing cancer or inhibiting metastasis of cancer susceptible to treatment in a subject at risk for developing cancer or metastasis of cancer, and method of identifying a candidate compound that selectively interferes with proliferation or viability of a cancer cell that has elevated levels of CCR5 and/or of at least one of its ligands.

  本公开内容部分涉及一种哺乳动物前列腺癌细胞系，该细胞系由至少一种或一组原代哺乳动物上皮细胞组成，这些细胞已被携带选自 c-Myc、Ha-Ras、NeuT、c-Src 及其组合的癌基因的逆转录病毒载体感染，并且在其中表达了所述基因。原态细胞系的应用，包括前列腺癌的免疫能力动物模型、体外生产永生化原始哺乳动物上皮细胞的方法、确定患有前列腺癌的人类受试者是否患有转移或是否有发生转移风险的方法、一种在有罹患癌症或癌症转移风险的受试者中预防癌症或抑制易受治疗的癌症转移的方法，以及一种鉴定候选化合物的方法，该候选化合物可选择性地干扰CCR5和/或其至少一种配体水平升高的癌细胞的增殖或存活。