Anticancer agent 83

• 常用名: Anticancer agent 83
• 英文名: Anticancer agent 83
• CAS号: 904815-29-8
• 分子量: 377.46
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₀H₁₉N₅OS
• 熔点: N/A
• 闪点: N/A

Anticancer agent 83用途

抗癌剂83是一种有效的抗癌剂,抑制LOX IMVI细胞生长,GI50值为0.15 mM。抗癌药物83降低线粒体膜电位并诱导DNA损伤,从而诱导白血病细胞凋亡[1]。

Anticancer agent 83名称

• 英文名: Anticancer agent 83

Anticancer agent 83生物活性

• 描述: 抗癌剂83是一种有效的抗癌剂,抑制LOX IMVI细胞生长,GI50值为0.15 mM。抗癌药物83降低线粒体膜电位并诱导DNA损伤,从而诱导白血病细胞凋亡[1]。
• 相关类别:
  信号通路 >> 细胞凋亡 >> 细胞凋亡
  研究领域 >> 癌症
• 体外研究: 抗癌剂83(化合物4a)(0.01-100μM；24小时)对人类结肠癌HCT116 p53表现出强烈活性−/− P53基因缺失的细胞(GI50=8.4μM)、人表皮样宫颈癌KB3-1(GI50=0.4μM),人卵巢癌Skov 3细胞(GI50=10μM)和人慢性粒细胞白血病K562细胞(GI50.=5.4μM)[1]。抗癌药物83(0.5μM；24小时)阻断Jurkat细胞中DNA的稳定性和诱导凋亡,并降低线粒体膜电位[1]。细胞活性测定[1]细胞株：人结肠癌HCT116 p53−/− P53基因缺失细胞、人表皮样宫颈癌KB3-1、人卵巢癌Skov 3细胞和人慢性粒细胞白血病K562细胞浓度：0.01、0.1、1、10、100μM培养时间：24小时结果：GI50s为8.4M(HCT116 P53−/−), 分别为7.4 M(KB3-1)、10 M(Skov 3)和5.4 M(K562)。免疫荧光[1]细胞株：Jurkat细胞浓度：0.5μM孵育时间：24小时结果：诱导Jurkat T细胞形态学改变(包括凋亡小体、膜泡、染色质凝集)和DNA片段化。
• 参考文献:

  [1]. Pokhodylo N, et al. Novel N-(4-thiocyanatophenyl)-1H-1,2,3-triazole-4-carboxamides exhibit selective cytotoxic activity at nanomolar doses towards human leukemic T-cells. Eur J Med Chem. 2022 Nov 5;241:114633.

Anticancer agent 83物理化学性质

• 分子式: C₂₀H₁₉N₅OS
• 分子量: 377.46
• InChIKey: YVZLYBOOUTVSFY-UHFFFAOYSA-N
• SMILES: Cc1c(C(=O)Nc2ccc(SC#N)cc2)nnn1-c1ccc(C(C)C)cc1

Anticancer agent 83靶点实验

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实验名称：Antiproliferative activity against human SR cells incubated for 48 hrs and measured b... 来源：ChEMBL 靶标：SR External Id：CHEMBL5110842

实验名称：Antiproliferative activity against human Malme-3M cells assessed as relative cell gro... 来源：ChEMBL 靶标：Malme-3M External Id：CHEMBL5110838

实验名称：Antiproliferative activity against human LOX IMVI cells incubated for 48 hrs and meas... 来源：ChEMBL 靶标：LOX IMVI External Id：CHEMBL5110839

实验名称：Antiproliferative activity against human NCI-H522 cells incubated for 48 hrs and meas... 来源：ChEMBL 靶标：NCI-H522 External Id：CHEMBL5110841

实验名称：Antiproliferative activity against human MDA-MB-468 cells assessed as relative cell g... 来源：ChEMBL 靶标：MDA-MB-468 External Id：CHEMBL5110834

实验名称：Antiproliferative activity against human HCC 2998 cells assessed as relative cell gro... 来源：ChEMBL 靶标：HCC 2998 External Id：CHEMBL5110835

实验名称：Antiproliferative activity against human COLO 205 cells assessed as relative cell gro... 来源：ChEMBL 靶标：COLO 205 External Id：CHEMBL5110836

实验名称：Antiproliferative activity against human A498 cells assessed as relative cell growth ... 来源：ChEMBL 靶标：A498 External Id：CHEMBL5110837

实验名称：Antiproliferative activity against human SF-295 cells assessed as relative cell growt... 来源：ChEMBL 靶标：SF-295 External Id：CHEMBL5110830

实验名称：Antiproliferative activity against human HL-60(TB) cells assessed as relative cell gr... 来源：ChEMBL 靶标：HL-60(TB) External Id：CHEMBL5110831

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