Tesevatinib | 781613-23-8

• 物质功能分类: 生物化工 - 生化试剂 - 激动剂抑制剂
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: Tesevatinib
• 英文别名: N-(3,4-dichloro-2-fluorophenyl)-7-((((3aR,5r,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl)-methyl)-oxy)-6-(methyloxy)quinazolin-4-amine；N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine；N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine；XL647；N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta-[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine
• CAS: 781613-23-8
• 化学式: C₂₄H₂₅Cl₂FN₄O₂
• 分子量: 491.393
• InChiKey: HVXKQKFEHMGHSL-QKDCVEJESA-N

物化性质

• 沸点：
  567.9±50.0 °C(Predicted)
• 密度：
  1.356
• 溶解度：
  DMF：10mg/mL； DMSO：10mg/mL；乙醇：10mg/mL

计算性质

• 辛醇/水分配系数(LogP)：
  5.79
• 重原子数：
  33.0
• 可旋转键数：
  6.0
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  59.51
• 氢给体数：
  1.0
• 氢受体数：
  6.0

安全信息

• 危险性防范说明：
  P261,P305+P351+P338
• 危险性描述：
  H302,H315,H319,H335
• 储存条件：
  2-8℃

制备方法与用途

应用

XL-647（Tesevatinib；XL-647；KD-019）是一种多靶点酪氨酸激酶抑制剂，其IC50值分别为：EGFR为0.3 nM、ErbB2为16 nM、KDR为1.5 nM、Flt4为8.7 nM 和 EphB4 为1.4 nM，有效抑制这些激酶的活性。

文献信息

• [EN] ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT
  申请人：NOVARTIS AG

  公开号：WO2016203432A1

  公开（公告）日：2016-12-22

  This application discloses anti-P-cadherin antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments, particularly antibody drug conjugates comprising anti-P-cadherin antibodies conjugated to auristatin analogs. The invention also relates to methods of treating cancer using the antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.

  该应用程序披露了抗P-钙粘蛋白抗体、其抗原结合片段，以及所述抗体或抗原结合片段的抗体药物偶联物，特别是包括与奥利司他汀类似物偶联的抗P-钙粘蛋白抗体的抗体药物偶联物。该发明还涉及使用抗体药物偶联物治疗癌症的方法。本文还披露了制备抗体、抗原结合片段和抗体药物偶联物的方法，以及将抗体和抗原结合片段用作诊断试剂的方法。
• Receptor-Type Kinase Modulators and Methods of Use
  申请人：Rice Kenneth D.

  公开号：US20160129032A1

  公开（公告）日：2016-05-12

  The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

  本发明提供了用于调节受体激酶活性的化合物，特别是ephrin和EGFR，并利用这些化合物及其药物组合物治疗由受体激酶活性介导的疾病的方法。由受体激酶活性介导的疾病包括但不限于部分表现为细胞增殖异常水平（即肿瘤生长）、程序性细胞死亡（凋亡）、细胞迁移和侵袭以及与肿瘤生长相关的血管生成的疾病。本发明的化合物包括“谱选择性”激酶调节剂，这些化合物抑制、调节和/或调节跨受体型酪氨酸激酶亚家族的信号传导，包括ephrin和EGFR。
• Receptor-type kinase modulators and methods of use
  申请人：Rice Kenneth D.

  公开号：US20090318373A1

  公开（公告）日：2009-12-24

  The present invention provides compounds for modulating receptor kinase activity, particularly ephrin and EGFR, and methods of treating diseases mediated by receptor kinase activity utilizing the compounds and pharmaceutical compositions thereof. Diseases mediated by receptor kinase activity include, but are not limited to, diseases characterized in part by abnormal levels of cell proliferation (i.e. tumor growth), programmed cell death (apoptosis), cell migration and invasion and angiogenesis associated with tumor growth. Compounds of the invention include “spectrum selective” kinase modulators, compounds that inhibit, regulate and/or modulate signal transduction across subfamilies of receptor-type tyrosine kinases, including ephrin and EGFR.

  本发明提供了用于调节受体激酶活性的化合物，特别是调节ephrin和EGFR的化合物，以及利用这些化合物和其制剂治疗由受体激酶活性介导的疾病的方法。由受体激酶活性介导的疾病包括但不限于部分以细胞增殖水平异常（即肿瘤生长）、程序性细胞死亡（凋亡）、细胞迁移和侵袭以及与肿瘤生长相关的血管生成为特征的疾病。本发明的化合物包括“谱选择性”激酶调节剂，这些化合物抑制、调节和/或调节受体型酪氨酸激酶亚家族之间的信号转导，包括ephrin和EGFR。
• Methods of using MEK inhibitors
  申请人：Lamb Peter

  公开号：US20080166359A1

  公开（公告）日：2008-07-10

  The present invention provides methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments.

  本发明提供了一种通过给予I式化合物或其药学上可接受的盐或溶剂与其他癌症治疗相结合的方法来治疗癌症的方法。
• PYRIDO [2, 3-D] PYRIMIDIN-7-ONE COMPOUNDS AS INHIBITORS OF P13K-ALPHA FOR THE TREATMENT OF CANCER
  申请人：Buhr Chris A.

  公开号：US20100209340A1

  公开（公告）日：2010-08-19

  The invention is directed to Compounds of Formula (I). The invention provides compounds that inhibit, regulate, and/or modulate P13K that are useful in the treatment of hyperproliferative diseases, such as cancer.

  该发明涉及式(I)化合物。该发明提供了抑制、调节和/或调控P13K的化合物，这些化合物在治疗高增殖性疾病，如癌症方面是有用的。