2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. ATP Synthase Reactive Oxygen Species (ROS) Apoptosis Ferroptosis
  4. Antitumor agent-217

Antitumor agent-217 是一种双线粒体靶向的抗癌剂。Antitumor agent-217 对膀胱癌细胞 J82 具有强效且选择性的抗增殖活性 (IC50 = 6.3 μM)，可抑制 J82 的集落形成与迁移。Antitumor agent-217 会在线粒体中积累，改变线粒体形态，减少 ATP 生成，提高 ROS 生成量并降低线粒体膜电位。Antitumor agent-217 可诱导膀胱癌细胞发生凋亡 (Apoptosis) 和铁死亡 (Ferroptosis)。Antitumor agent-217 可用于膀胱癌的研究。

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Antitumor agent-217

Antitumor agent-217 Chemical Structure

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Antitumor agent-217 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

Antitumor agent-217 is a dual mitochondria-targeted anticancer agent. Antitumor agent-217 exhibits potent and selective antiproliferative activity against bladder cancer cell line J82 (IC50 = 6.3 μM), and inhibits colony formation and migration of J82 cells. Antitumor agent-217 accumulates in mitochondria, alters mitochondrial morphology, reduces ATP production, increases ROS generation and decreases mitochondrial membrane potential. Antitumor agent-217 induces apoptosis (Apoptosis) and ferroptosis (Ferroptosis) in bladder cancer cells. Antitumor agent-217 can be used for the research of bladder cancer[1].

体外研究
(In Vitro)

Antitumor agent-217 (化合物 7f) (Range of concentrations; 72 h) 可抑制 OVCAR3、SKOV3、J82、T24 和 A549 癌细胞的活力，其中对 J82 细胞的效力最强 (IC50 = 6.3 μM)，且相对于正常 SV-HUC-1 细胞具有高选择性[1]。
Antitumor agent-217 (1.5-6 μM; 6-8 days) 可剂量依赖性地抑制 J82 膀胱癌细胞的集落形成[1]。
Antitumor agent-217 (1.5-6 μM; 24-48 h) 可剂量依赖性地抑制 J82 膀胱癌细胞的迁移[1]。
Antitumor agent-217 (10 μM; 4 h) 在 J82 膀胱癌细胞的线粒体中积累[1]。
Antitumor agent-217 (8 μM; 48 h) 可破坏 J82 膀胱癌细胞的线粒体形态，引发线粒体肿胀、膜破裂及嵴丢失[1]。
Antitumor agent-217 (2-8 μM; 48 h) 剂量依赖性地降低 ATP 生成和线粒体膜电位，并增加 J82 膀胱癌细胞中的细胞内 ROS 水平[1]。
Antitumor agent-217 (2-8 μM; 48 h) 可通过上调促凋亡蛋白 BAX、下调抗凋亡蛋白 BCL-2，在 8 μM 浓度下诱导 J82 膀胱癌细胞发生凋亡[1]。
Antitumor agent-217 (2-8 μM; 48 h) 可通过提高脂质过氧化水平和 MDA 水平、降低 GSH 水平并下调 NRF2/SLC7A11/GPX4 信号轴，诱导 J82 膀胱癌细胞发生铁死亡[1]。

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

Antitumor agent-217 相关抗体:

Cell Proliferation Assay[1]

Cell Line: J82 human bladder cancer cells
Concentration: 1.5, 3, 6 μM
Incubation Time: 6-8 days
Result: Dose-dependently inhibited colony formation of J82 cells, with significant inhibition at all tested concentrations compared to untreated controls.
Showed slightly greater inhibitory potency than cisplatin at equal concentrations.

Cell Migration Assay [1]

Cell Line: J82 human bladder cancer cells
Concentration: 1.5, 3, 6 μM
Incubation Time: 24 h, 48 h
Result: Significantly reduced the migration ability of J82 cells, with dose-dependent inhibition of wound closure at 24 and 48 h compared to untreated controls.
Exhibited an inhibitory effect comparable to that of cisplatin.

Apoptosis Analysis[1]

Cell Line: J82 human bladder cancer cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
Result: Induced 5.02% early apoptosis and 47.5% late apoptosis in J82 cells at 8 μM, with total apoptosis reaching ~52.5%.
Dose-dependently upregulated pro-apoptotic BAX protein and downregulated anti-apoptotic BCL-2 protein, with the BAX/GAPDH ratio increasing to ~1.7 and the BCL-2/GAPDH ratio decreasing to ~0.5 at 8 μM compared to control.
分子量

668.99

Formula

C32H36BrClN5O2P
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

Antitumor agent-217 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Antitumor agent-217Antitumor agent217Antitumor agent 217ATP SynthaseReactive Oxygen Species (ROS)ApoptosisFerroptosisSKOV3SV-HUC-1J82ferroptosisOVCAR3bladder cancer cellsmitochondriaapoptosisT24A549Inhibitorinhibitorinhibit

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