1. Photosensitizer-9

Photosensitizer-9 是一种基于铱 (III) 的光敏剂,具有抗黑色素瘤活性。Photosensitizer-9 具备显著的光毒性 (IC50=0.98 μM) 与理想的光毒性指数 (PI=3.05)。Photosensitizer-9 在光照下产生大量不依赖氧气的细胞内•OH。Photosensitizer-9 可在缺氧条件下介导光动力疗法,协同激活黑色素瘤细胞中的 PANoptosis (通过上调剪切型 Caspase-3GSDMD-Np-MLKL)、铁死亡 (ferroptosis) (通过破坏 GSH-GPX4-LPO 轴)、凋亡 (apoptosis)、焦亡 (pyroptosis)、坏死性凋亡。Photosensitizer-9 在缺氧条件下通过促进损伤相关分子模式的释放诱导免疫原性细胞死亡,提高树突状细胞成熟率。Photosensitizer-9 可降低荷黑色素瘤小鼠的肿瘤体积。Photosensitizer-9 可用于黑色素瘤的相关研究。

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Photosensitizer-9

Photosensitizer-9 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Photosensitizer-9 is an iridium (III)-based photosensitizer with anti-melanoma activity. Photosensitizer-9 exhibits significant phototoxicity (IC50=0.98 μM) and an ideal phototoxicity index (PI=3.05). Under light irradiation, Photosensitizer-9 generates large amounts of intracellular •OH in an oxygen-independent manner. Photosensitizer-9 mediates photodynamic therapy under hypoxic conditions and synergistically activates PANoptosis (by upregulating cleaved Caspase-3, GSDMD-N, p-MLKL), ferroptosis (by disrupting the GSH-GPX4-LPO axis), apoptosis, pyroptosis and necroptosis in melanoma cells. Photosensitizer-9 induces immunogenic cell death by promoting the release of damage-associated molecular patterns under hypoxic conditions and increases the maturation rate of dendritic cells. Photosensitizer-9 reduces tumor volume in melanoma-bearing mice. Photosensitizer-9 is applicable to relevant studies on melanoma[1].

体外研究
(In Vitro)

Photosensitizer-9 (Ir1) (500 nM; 24 h cell treatment, 3 min light exposure) 在光照下可于 B16-F10 细胞中产生大量不依赖氧气的细胞内•OH,在缺氧环境下,•OH 是驱动其光动力效应的主要 ROS 亚型[1]
Photosensitizer-9 (0.125-10 μM; 24 h post-light/dark incubation) 对 B16-F10 细胞表现出强效、不依赖氧气的光毒性,且暗毒性较低,其抗缺氧活性主要由•OH 的产生驱动[1]
Photosensitizer-9 (2 μM; 24 h cell treatment, 3 min light exposure) 可在缺氧条件下介导光动力疗法,协同激活 B16-F10 细胞中的 PANoptosis (通过上调剪切型 Caspase-3、GSDMD-N、p-MLKL)、铁死亡 (通过破坏 GSH-GPX4-LPO 轴)、凋亡、焦亡、坏死性凋亡[1]
Photosensitizer-9 (500 nM-2 μM; 24 h cell treatment/DC co-culture, 3 min light exposure) 可介导光动力疗法,在常氧和低氧条件下诱导 B16-F10 细胞发生免疫原性细胞死亡 (ICD)(ATP 释放、CRT 暴露、HSP70/HMGB1 分泌),进而在体外促进骨髓来源树突状细胞 (DC) 的成熟[1]

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

Cell Viability Assay[1]

Cell Line: B16-F10 cells
Concentration: 0.125-10 μM (normoxia/hypoxia viability assay); 700 nM (normoxia scavenger assay); 2 μM (hypoxia scavenger assay)
Incubation Time: 24 h (post-light/dark incubation); 3 min (light exposure)
Result: Exhibited an IC50 of 0.54 μM and a phototoxic index (PI) of 13.48 under normoxia (light).
Reduced cell viability to 3% at 5 μM under normoxia (light) vs.
92% in dark.
Showed an IC50 of 0.98 μM and a phototoxic index (PI) of 3.06 under hypoxia (light).
Enabled restoration of cell viability from 8% to 43% under hypoxia when cells were treated with D-mannitol.

Immunofluorescence[1]

Cell Line: B16-F10 cells
Concentration: 500 nM
Incubation Time: 24 h cell treatment, 3 min light exposure
Result: Produced a strong green dichlorofluorescein (DCF) fluorescence signal, but did not elicit a noticeable fluorescence signal in dark environments.
体内研究
(In Vivo)

Photosensitizer-9 (25 μM,50 μL;瘤内注射; 2 次 (day 0, day 4)) 可使小鼠黑色素瘤体积减少 89%,将肿瘤转化为热免疫原性表型,并激活系统性抗肿瘤免疫,且未观察到副作用[1]

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

Animal Model: C57BL/6 J (female, 6-8 weeks old, 18-23 g, subcutaneous injection of 5×105 B16-F10 melanoma cells)[1]
Dosage: 25 μM,50 μL
Administration: intratumoral injection; 2 doses (day 0, day 4); followed by broad-spectrum white LED light irradiation at 50 mW/cm2 for 12 minutes with 1-minute pause every 3 minutes post-injection
Result: Achieved an 89% reduction in tumor volume.
Induced significant tumor cell destruction, reduced tumor cell density, and decreased proliferative capacity.
Increased splenic CD8+ T cells to ~18% and splenic CD4+ T cells to ~21% relative to control groups.
Increased tumor-infiltrating CD8+ and CD4+ T cells.
Elevated serum TNF-α to ~650 pg/mL and IFN-γ to ~28 pg/mL relative to control groups.
Converted immunosuppressed "cold" tumors to inflamed "hot" phenotypes.
Caused no significant body weight loss or histopathological lesions in vital organs.
分子量

1184.29

Formula

C50H34F6IrN6PS42+

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

Photosensitizer-9 相关分类

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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.

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产品名称:
Photosensitizer-9
目录号:
HY-182066
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