2. Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Apoptosis Reactive Oxygen Species
  4. Antitumor photosensitizer-5

Antitumor photosensitizer-5 (Ru2) 是一种有效靶向肿瘤线粒体的光敏剂，对 A549 细胞光毒性的 IC50 为 0.3 μM。在 460 nm 光照下，Antitumor photosensitizer-5 诱导活性氧的生成和 NADH 的耗竭，进而导致线粒体损伤并活化 caspase-3，诱导细胞凋亡并抑制细胞迁移。Antitumor photosensitizer-5 具有阻止恶性肿瘤生长的潜力，因此显示出应用于光动力治疗的潜力。

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Antitumor photosensitizer-5 Chemical Structure

Antitumor photosensitizer-5 Chemical Structure

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Antitumor photosensitizer-5 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 photosensitizer-5 (Ru2) is a photosensitizer which effectively target tumor mitochondria with an IC50 of 0.3 μM for phototoxicity to A549 cells. Under 460 nm light irradiation, antitumor photosensitizer-5 induces the generation of reactive oxygen species and NADH depletion, causes mitochondrial damage and activation of caspase-3, inducing apoptosis and suppressing cell migration. Antitumor photosensitizer-5 has the potential to prevent the growth of malignant tumors, therefore, shows the potential to be applied to photodynamic therapy[1].

IC50 & Target

Nicotinamide adenine dinucleotide (NADH)[1]
体外研究
(In Vitro)

Antitumor photosensitizer-5 (10 μM, 4 h) 可使生物素受体阳性的 A549 细胞荧光信号显著增加 (32.08 倍)，而生物素受体阴性的 BHK 细胞荧光信号增加可忽略 (7.35 倍) [1]。
Antitumor photosensitizer-5 (0.391-100 μM, 24 h) 在 BHK 细胞和 A549 细胞中均表现出光毒性，在 100 μM 无光条件下表现出最小的细胞毒性，细胞存活率超过 75%[1]。
Antitumor photosensitizer-5 (10 μM, 4 h) 与线粒体探针 Mito-Tracker Green 的 Pearson 共定位系数为 0.87[1]。
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h) 在 460 nm 光照射 15 min 后，线粒体膜电位探针荧光强度比呈浓度依赖性降低，表明线粒体损伤，而 ROS 探针荧光强度呈浓度依赖性增加，表明 ROS 的高效生成[1]。
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h) 在光照后可引起 A549 细胞发生凋亡，在黑暗条件下细胞凋亡水平基本不变，光照条件下使活化 caspase-3 与 DNA 迁移损伤增加，使细胞 NADH 含量降低[1]。
Antitumor photosensitizer-5 (0.15-0.6 μM, 24 h/48 h) 在 460 nm 光照后抑制 A549 细胞的迁移[1]。

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

Antitumor photosensitizer-5 相关抗体:

Cell Viability Assay[1]

Cell Line: BHK, A549
Concentration: 0.195, 0.391, 0.781, 1.563, 3.125, 6.250, 12.5, 25, 50, 100 μM
Incubation Time: 4 h in dark + 15 min in light or dark + 20 h in dark
Result: Exhibited phototoxicity in both BHK cells and A549 cells, but was more phototoxic in A549 cells (A549 cell viability < 40% under 0.391 μM while BHK cell viability < 40% under 6.25 μM), revealed minimal cytotoxicity in the absence of light with over 75 % cell viability under 100 μM.

Apoptosis Analysis[1]

Cell Line: A549
Concentration: 0.15, 0.3, 0.6 μM
Incubation Time: 4 h in dark + 15 min in light or dark + 20 h in dark
Result: Increased the percentage of early and late apoptotic cells in A549 in a concentration-dependent manner under the 460 nm light condition. Conversely, under dark conditions, the percentage of early and late apoptotic cells in treated A549 cells remained virtually unchanged.

Cell Migration Assay [1]

Cell Line: A549
Concentration: 0.15, 0.3, 0.6 μM
Incubation Time: 4 h in dark + 15 min in light or dark + 20 h/44 h in dark
Result: Displayed a significant concentration-dependent inhibition of wound healing in A549 cells under 460 nm light compared to cells kept in the dark.
体内研究
(In Vivo)

Antitumor photosensitizer-5 (10 mg/kg, i.tu. 一次，24 d) 在 460 nm 光照射后显著抑制肿瘤生长，且对正常器官无严重不良影响[1]。

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

Animal Model: BALB/c nude female mice (6–8 weeks old) , Human lung adenocarcinoma epithelial A549 cells[1]
Dosage: 10 mg/kg
Administration: intratumoral injection (i.tu.) for once
Result: Suppressed the tumor growth remarkably in the light group while tumors in the dark or control groups grow rapidly during the same period.
Caused severe apoptosis and disruption of the tumor structure in the tumor of light group while the tumors in the other group showed no obvious tissue damage, normal organs such as the heart, liver, spleen, lung, and kidney did not exhibit significant pathological abnormalities or inflammatory lesions.
分子量

1289.04

Formula

C53H43F12N11O2P2RuS
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 photosensitizer-5 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Antitumor photosensitizer-5Antitumor photosensitizer5Antitumor photosensitizer 5ApoptosisReactive Oxygen SpeciesA549 cellMDAMB-231 cellMCF-7 cellBHK cellsBALB/c nude micesinglet oxygenreactive oxygen speciesNADHcancermitochondriaRuthenium(II) complexesAggregation-induced emissioncaspase-3Photodynamic therapyInhibitorinhibitorinhibit

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