LQZ-7I

• 常用名: LQZ-7I
• 英文名: LQZ-7I
• CAS号: 195822-23-2
• 分子量: 348.35
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₄F₂N₄
• 熔点: N/A
• 闪点: N/A

LQZ-7I用途

LQZ-7I 是一种靶向 survivin 的抑制剂。LQZ-7I 抑制生存素二聚化。LQZ-7I 口服有效抑制异种移植肿瘤生长并诱导肿瘤中生存素的损失。

LQZ-7I名称

• 中文名: N2,N3-双(4-氟苯基)喹喔啉-2,3-二胺
• 英文名: LQZ-7I

LQZ-7I生物活性

• 描述: LQZ-7I 是一种靶向 survivin 的抑制剂。LQZ-7I 抑制生存素二聚化。LQZ-7I 口服有效抑制异种移植肿瘤生长并诱导肿瘤中生存素的损失。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞凋亡 >> 存活
• 靶点实验:

  Survivin[1]

• 体外研究: 与母体化合物LQZ-7相比,LQZ-7I提高了对C4-2细胞的3.1µM和对PC-3细胞的4.8µM的细胞毒性[1]。LQZ-7I(10µM；0-6小时)治疗可降低survivin的表达。然而,LQZ-7I并不降低XIAP、CIAP1和CIAP2的表达。LQZ-7I可能对其预期目标survivin具有选择性[1]。Western Blot分析[1]细胞系：PC-3或C4-2细胞浓度：10µM孵育时间：0-6h结果：survivin表达降低。
• 体内研究: LQZ-7I(100mg/kg；隔日口服,共10个疗程)显著抑制肿瘤生长,对小鼠无明显不良影响[1]。动物模型：6周龄雄性NSG小鼠[1]剂量：100mg/kg；200µL溶媒(90%玉米油/10%二甲基亚砜)给药：隔日灌胃,共10次。结果：小鼠体重和主要器官湿重无明显变化,对肿瘤生长无明显不良影响在研究的最后。
• 参考文献:

  [1]. Robert Peery,et al. Synthesis and Identification of a Novel Lead Targeting Survivin Dimerization for Proteasome-Dependent Degradation. J Med Chem. 2020 Jun 9.

LQZ-7I物理化学性质

• 分子式: C₂₀H₁₄F₂N₄
• 分子量: 348.35
• InChIKey: DKPCKOKYSVPFEB-UHFFFAOYSA-N
• SMILES: Fc1ccc(Nc2nc3ccccc3nc2Nc2ccc(F)cc2)cc1
• 储存条件: 2-8°C，干燥，密封

LQZ-7I安全信息

• 危害码 (欧洲): Xi

LQZ-7I靶点实验

查看更多实验

实验名称：Antitumor activity against human PC3 cells xenografted in NSG mouse assessed as reduc... 来源：ChEMBL 靶标：PC-3 External Id：CHEMBL4618207

实验名称：Toxicity in NSG mouse xenografted in human PC3 cells assessed as effect on stomach we... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4618206

实验名称：In vivo inhibition of survivin in NSG mouse xenografted in human PC3 cells assessed a... 来源：ChEMBL 靶标：Baculoviral IAP repeat-containing protein 5 External Id：CHEMBL4618209

实验名称：Antitumor activity against human PC3 cells xenografted in NSG mouse assessed as chang... 来源：ChEMBL 靶标：PC-3 External Id：CHEMBL4618208

实验名称：A screen for compounds that inhibit the activity of LtaS in Staphylococcus aureus 来源：ICCB-Longwood/NSRB Screening Facility, Harvard Medical School External Id：HMS979

实验名称：Solubility of the compound in corn oil 来源：ChEMBL 靶标：N/A External Id：CHEMBL4618211

实验名称：In vivo inhibition of survivin in NSG mouse xenografted in human PC3 cells assessed a... 来源：ChEMBL 靶标：Baculoviral IAP repeat-containing protein 5 External Id：CHEMBL4618210

实验名称：Induction of apoptosis in human PC3 cells at 3 uM measured after 48 hrs by Annexin V-... 来源：ChEMBL 靶标：PC-3 External Id：CHEMBL4618199

实验名称：Induction of apoptosis in human C4-2 cells at 3 uM measured after 48 hrs by Annexin V... 来源：ChEMBL 靶标：LNCaP C4-2 External Id：CHEMBL4618198

实验名称：Toxicity in NSG mouse xenografted in human PC3 cells assessed as effect on body weigh... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4618201

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LQZ-7I英文别名

• MFCD00607076