LMP744盐酸盐

• 常用名: LMP744盐酸盐
• 英文名: LMP744 hydrochloride
• CAS号: 308246-57-3
• 分子量: 488.91800
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₅ClN₂O₇
• 熔点: N/A
• 闪点: N/A

LMP744盐酸盐用途

LMP744 hydrochloride (MJ-III65 hydrochloride) 是一种 DNA 嵌和剂,是 拓扑异构酶 1 (Top1) 抑制剂,具有抗肿瘤活性。

LMP744盐酸盐名称

• 中文名: LMP744盐酸盐
• 英文名: 6-[3-[(2-Hydroxyethyl)amino]propyl]-5,11-diketo-2,3-dimethoxy-8,9-(methylenedioxy)-11H-indeno[1,2-c]isoquinoline Hydrochloride

LMP744盐酸盐生物活性

• 描述: LMP744 hydrochloride (MJ-III65 hydrochloride) 是一种 DNA 嵌和剂,是 拓扑异构酶 1 (Top1) 抑制剂,具有抗肿瘤活性。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 细胞周期/DNA损伤 >> 拓扑异构酶
• 靶点实验:

  Top1[1].

• 体外研究: LMP744(MJ-III-65)对NCI60细胞的GI50值为0.1μM[1]。 LMP744(0.1-5μM,3天)诱导细胞周期的S期和G2期细胞的剂量依赖性积累[1]。细胞毒性测定[1]细胞系：P388和P388 Top1缺陷型鼠白血病细胞浓度：0.1-100μM孵育时间：3天结果：诱导剂量依赖性细胞在细胞周期的S期和G2期积累
• 体内研究: MJ-III-65(10-50mg/kg)静脉推注,每周一次,在针对人A253和FaDu肿瘤异种移植物的中度活性的裸鼠中施用4周,没有显着毒性[2]。动物模型：无胸腺裸鼠(nu/nu,雌性,20-25g,8-12周龄)移植A253和FaDu人头颈部异种移植物[2]。剂量：10,25或50mg/kg /周,4周给药：静脉推注尾静脉结果：对人A253和FaDu肿瘤异种移植物有中等活性,无明显毒性
• 参考文献:

  [1]. Antony S, et al. Bisindenoisoquinoline bis-1,3-{( 5,6-dihydro-5,11-diketo-11H-indeno [1,2-c]isoquinoline)-6-propylamino}propane bis(trifluoroacetate) (NSC 727357), a DNA intercalator and topoisomerase inhibitor with antitumor activity. Mol Pharmacol. 2006 Sep;70(3):1109-20.

  [2]. Antony S, et al. Cellular topoisomerase I inhibition and antiproliferative activity by MJ-III-65 (NSC 706744), an indenoisoquinoline topoisomerase I poison. Mol Pharmacol. 2005 Feb;67(2):523-30.

LMP744盐酸盐物理化学性质

• 分子式: C₂₄H₂₅ClN₂O₇
• 分子量: 488.91800
• 精确质量: 488.13500
• PSA: 108.25000
• LogP: 3.12370
• InChIKey: POXWLZDVWCKKEX-UHFFFAOYSA-N
• SMILES: COc1cc2c3c(n(CCCNCCO)c(=O)c2cc1OC)-c1cc2c(cc1C3=O)OCO2.Cl
• 储存条件: 2-8℃

LMP744盐酸盐靶点实验

查看更多实验

实验名称：Antiproliferative activity was determined for 50% growth inhibition against human ren... 来源：ChEMBL 靶标：SN12C External Id：CHEMBL802463

实验名称：Inhibitory activity of compound against human recombinant DNA topoisomerase I mediate... 来源：ChEMBL 靶标：DNA topoisomerase 1 External Id：CHEMBL665551

实验名称：Mean graph mid point for growth inhibition of human cancer cell lines 来源：ChEMBL 靶标：Panel (Carcinoma cell lines) External Id：CHEMBL826818

实验名称：Growth inhibitory activity against human breast MDA-MB-435 cell line 来源：ChEMBL 靶标：MDA-MB-435 External Id：CHEMBL836386

实验名称：Growth inhibitory activity against human CNSSF-539 cell line 来源：ChEMBL 靶标：NON-PROTEIN TARGET External Id：CHEMBL825887

实验名称：Antiproliferative activity was determined for 50% growth inhibition against human col... 来源：ChEMBL 靶标：HCT-116 External Id：CHEMBL690486

实验名称：Antiproliferative activity was determined for 50% growth inhibition against human ova... 来源：ChEMBL 靶标：OVCAR-3 External Id：CHEMBL747106

实验名称：Growth inhibitory activity against human renal SN12C cell line 来源：ChEMBL 靶标：SN12C External Id：CHEMBL836365

实验名称：Growth inhibitory activity against human lung HOP-62 cell line 来源：ChEMBL 靶标：HOP-62 External Id：CHEMBL836364

实验名称：Induction of topoisomerase I mediated DNA cleavage; Greater activity than parent comp... 来源：ChEMBL 靶标：DNA topoisomerase 1 External Id：CHEMBL832068

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LMP744盐酸盐英文别名

• 5H-[1,6]indeno[1,2-c]isoquinoline-5,12(6H)-dione,6-[3-[(2-hydroxyethyl)amino]propyl]-2,3-dimethoxy-,monohydrochloride