2. Apoptosis
  3. Ferroptosis Apoptosis
  4. anti-NSCLC agent-2

anti-NSCLC agent-2 (compound 6o) 是一种 SLC7A11 和 GPX4 抑制剂，可降低铁死亡关键调控因子 SLC7A11 和 GPX4 的表达。anti-NSCLC agent-2 可破坏氧化还原稳态、耗竭谷胱甘肽、积累脂质过氧化物，并诱导非小细胞肺癌细胞发生铁死亡。anti-NSCLC agent-2 可用于非小细胞肺癌的相关研究。

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anti-NSCLC agent-2

anti-NSCLC agent-2 Chemical Structure

CAS No. : 3063042-21-4

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anti-NSCLC agent-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

anti-NSCLC agent-2 (compound 6o) is a SLC7A11 and GPX4 inhibitor that reduces the expression of ferroptosis key regulators SLC7A11 and GPX4. anti-NSCLC agent-2 disrupts redox homeostasis, depletes glutathione, accumulates lipid peroxides, and induces ferroptosis in non-small cell lung cancer cells. anti-NSCLC agent-2 is applicable to research related to non-small cell lung cancer[1].

体外研究
(In Vitro)

anti-NSCLC agent-2 (compound 6o) (10-160 nM; 48 h) 可强效抑制 A549、H1299、H2030、H1975、A549/T 及 A549/CDDP 非小细胞肺癌细胞系的增殖，其 IC50 值范围为 1.54 nM 至 11.72 nM，且在有效抑瘤浓度下对正常 HUVECs 无明显毒性[1]。
anti-NSCLC agent-2 (compound 6o) (100 μM; 2.5 h) 可在 A549 细胞中释放 10.02 μM 的一氧化氮[1]。
anti-NSCLC agent-2 (50 nM; 48 h) 对 A549 和 A549/CDDP 细胞具有抗增殖活性，该活性依赖于一氧化氮；正如通过血红蛋白清除作用呈浓度依赖性逆转这一结果所证实的[1]。
Anti-NSCLC agent-2 (100 nM; 48 h) 对 A549 和 A549/CDDP 细胞具有抗增殖活性，该活性依赖于铁死亡；正如 Ferrostatin-1 可浓度依赖性地逆转该活性这一结果所示[1]。
anti-NSCLC agent-2 (特定浓度；4 h) 可呈剂量依赖性增加 A549 和 A549/CDDP 细胞中的亚铁离子蓄积，支持其诱导铁死亡的作用[1]。
anti-NSCLC agent-2 (特定浓度；4 h) 可呈剂量依赖性地诱导 A549 和 A549/CDDP 细胞发生脂质过氧化，其绿/红荧光比值分别升高至 1.51 和 1.10[1]。
anti-NSCLC agent-2 (15-60 nM; 12 h) 可通过铁死亡依赖的机制，以剂量依赖方式下调 A549 和 A549/CDDP 细胞中 SLC7A11 与 GPX4 的蛋白表达[1]。
anti-NSCLC agent-2 (20-80 nM; 3-12 h) 可呈剂量和时间依赖性升高 A549 细胞与 A549/CDDP 细胞内的活性氧水平[1]。
anti-NSCLC agent-2 (40-80 nM; 12 h) 可呈剂量依赖性地消耗 A549 和 A549/CDDP 细胞内的谷胱甘肽并降低 GSH/GSSG 比值，从而破坏氧化还原稳态[1]。
anti-NSCLC agent-2 (20-80 nM; 4 h) 可提高 A549 细胞 (20 nM) 和 A549/CDDP 细胞 (80 nM) 中的线粒体一氧化氮水平[1]。
anti-NSCLC agent-2 (特定浓度；4 h) 可呈剂量依赖性诱导 A549 和 A549/CDDP 细胞的线粒体膜电位崩溃[1]。
anti-NSCLC agent-2 (特定浓度；4 h) 可呈剂量依赖性地升高 A549 和 A549/CDDP 细胞中的线粒体活性氧 (超氧化物) 水平[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

anti-NSCLC agent-2 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549, H1299, H2030, H1975, A549/T, A549/CDDP, HUVECs
Concentration: 20 nM (initial screening); 8 concentration gradients (IC50 determination); 10-160 nM (HUVEC viability assessment)
Incubation Time: 48 h
Result: Showed potent nanomolar antiproliferative activity with IC50 values of 6.29 nM (A549), 1.56 nM (H1299), 2.30 nM (H2030), 1.54 nM (H1975), 1.69 nM (A549/T), and 11.72 nM (A549/CDDP).
Showed no statistically significant reduction in HUVEC viability compared to blank controls at 10-160 nM.

Cell Proliferation Assay[1]

Cell Line: A549, A549/CDDP
Concentration: 50 nM (compound 6o); 0, 6.25, 12.5, 25 μM (hemoglobin pre-treatment)
Incubation Time: 4 h (hemoglobin pre-treatment); 48 h (compound 6o incubation)
Result: Decreased in antiproliferative effect with increasing hemoglobin concentration.
Dropped below 15% in inhibition rate at 25 μM hemoglobin.

Cell Proliferation Assay[1]

Cell Line: A549, A549/CDDP
Concentration: 100 nM (compound 6o); 0, 75, 150, 300 nM (Ferrostatin-1)
Incubation Time: 48 h
Result: Decreased in proliferation inhibition rate with increasing Ferrostatin-1 concentration in a concentration-dependent manner.
Lost almost all inhibitory activity at 300 nM Ferrostatin-1, with cell viability >95%.

Western Blot Analysis[1]

Cell Line: A549, A549/CDDP
Concentration: 15, 30 nM (A549); 30, 60 nM (A549/CDDP); 300 nM (Fer-1 for reversal)
Incubation Time: 12 h (compound 6o treatment)
Result: Dose-dependently downregulated the expression of SLC7A11 and GPX4 in both cell lines.
Fully reversed this downregulation in the presence of 300 nM Fer-1.
体内研究
(In Vivo)

anti-NSCLC agent-2 (compound 6o) (5-10 mg/kg；静脉注射；每 2 天 1 次；共 20 天) 对顺铂耐药的 A549/CDDP 异种移植物具有剂量依赖性的体内抗增殖活性，其中 10 mg/kg 剂量的疗效优于 10 mg/kg 顺铂，同时安全性良好，未观察到器官毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (female, SPF-grade, cisplatin-resistant NSCLC xenograft model)[1]
Dosage: 5 mg/kg; 10 mg/kg
Administration: i.v. (tail vein); once every 2 days; 20 days
Result: Significantly reduced tumor volume compared to vehicle control at 5 mg/kg.
Reduced final tumor weight compared to both vehicle control and 10 mg/kg cisplatin group at 5 mg/kg.
Achieved the greatest tumor volume reduction among all treatment groups at 10 mg/kg.
Reduced final tumor weight significantly lower than vehicle control and 10 mg/kg cisplatin group at 10 mg/kg.
Showed no significant body weight loss or behavioral abnormalities in either dose group.
Caused no treatment-related histopathological damage to heart, liver, spleen, lung, and kidney as observed via H&E staining.
分子量

603.43

Formula

C27H20Cl2N2O8S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

anti-NSCLC agent-2 相关分类

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Keywords:

anti-NSCLC agent-23063042-21-4FerroptosisApoptosisH1975GPX4H2030HUVECsSLC7A11ferroptosisA549H1299hERG channelnonsmall cell lung cancer cellsInhibitorinhibitorinhibit

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