4-[8-Methoxy-2-(oxan-4-yl)-1-(1-phenylethyl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole | 1300735-33-4

• 英文名称: 4-[8-Methoxy-2-(oxan-4-yl)-1-(1-phenylethyl)imidazo[4,5-c]quinolin-7-yl]-3,5-dimethyl-1,2-oxazole
• CAS: 1300735-33-4
• 化学式: C₂₉H₃₀N₄O₃
• 分子量: 482.582
• InChiKey: QEOHUTWVBBVSSC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5
• 重原子数：
  36
• 可旋转键数：
  5
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.34
• 拓扑面积：
  75.2
• 氢给体数：
  0
• 氢受体数：
  6

文献信息

• MECHANISM OF RESISTANCE TO BET BROMODOMAIN INHIBITORS
  申请人：Dana-Farber Cancer Institute, Inc.

  公开号：US20200368248A1

  公开（公告）日：2020-11-26

  The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MED1) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.