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细胞凋亡 细胞凋亡 自噬 干细胞 帕金森与阿尔茨海默症 肿瘤干细胞 Hippo
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自噬 TEAD Antiparasitic 细胞凋亡诱导剂 凋亡
/ Verteporfin

维替泊芬 /Verteporfin {[allProObj[0].p_purity_real_show]}

货号：A138297 同义名： CL 318952;BPD-MA

Verteporfin（维替泊芬)是一种YAP抑制剂，有效地破坏YAP-TEAD相互作用并诱导细胞凋亡，同时作为自噬抑制剂，通过阻止自噬体的形成来特异性阻断自噬的早期阶段。Verteporfin作为一种光敏剂，能够在光照下生成活性氧物质，IC50 值为 0.6 nM。Verteporfin 具有抗肿瘤和抗血管生成作用，可用于光动力疗法和年龄相关性黄斑变性的研究。

Verteporfin 化学结构 CAS号：129497-78-5
Verteporfin 化学结构
CAS号：129497-78-5
Verteporfin 3D分子结构
CAS号：129497-78-5
Verteporfin 化学结构 CAS号：129497-78-5
Verteporfin 3D分子结构 CAS号：129497-78-5
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Verteporfin 纯度/质量文件 产品仅供科研

货号：A138297 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		97%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 hydrochloride ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		97%
Lys05 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Verteporfin 生物活性

靶点

  • VDA
描述 Verteporfin (CL 318952) is utilized as a photosensitizer in photodynamic therapy aimed at eradicating abnormal blood vessels in the eye, particularly in conditions like age-related macular degeneration. It also functions as a YAP inhibitor, effectively disrupting YAP-TEAD interactions and inducing apoptosis in cells[1]. Additionally, Verteporfin acts as an autophagy inhibitor, specifically blocking the early stages of autophagy by preventing autophagosome formation[3].
体内研究

In vivo studies have demonstrated that Verteporfin, administered at 10 mg/kg through c.s.c., significantly reduces the leukemia cell ratio in combination with BMS-354825. This combined therapy further decreases the number of leukemia cells found in the spleen[1].
体外研究

In a specific PDX-cell screening, Verteporfin demonstrated varying levels of efficacy. The concentrations required to achieve 50% growth inhibition (GI50) in PhLO, PhLH, and PhLK cells were 228 nM, 395 nM, and 538 nM, respectively. For other cell types such as ALL-1, TCC-Y/sr, and NPhA1, the GI50 values were significantly higher, at 3.93 μM, 2.11 μM, and 5.61 μM, respectively. The presence of glutathione (GSH) notably decreased the sensitivity of two out of three PDX cell models to Verteporfin. Furthermore, Verteporfin has been shown to lower the mitochondrial membrane potential in PDX cells[1].

Verteporfin also plays a role in reducing PTX-resistance in HCT-8/T cells by downregulating YAP expression. The combined use of Verteporfin with NSC 125973 exhibits synergistic effects in inhibiting YAP and enhancing cytotoxicity against HCT-8/T cells[2].
作用机制 Verteporfin is transported in the plasma primarily by lipoproteins and once been activated by light in the presence of oxygen, highly reactive, short-lived singlet oxygen and reactive oxygen radicals are generated. Light activation of verteporfin can locally damage neovascular endothelium, resulting in vessel occlusion. Damaged endothelium is known to release procoagulant and vasoactive factors through the lipo-oxygenase (leukotriene) and cyclo-oxygenase (eicosanoids such as thromboxane) pathways, resulting in platelet aggregation, fibrin clot formation and vasoconstriction. Verteporfin appears to somewhat preferentially accumulate in neovasculature, including choroidal neovasculature. However, animal models indicate that the drug is also present in the retina. As singlet oxygen and reactive oxygen radicals are cytotoxic, Verteporfin can also be used to destroy tumor cells. https://www.drugbank.ca/drugs/DB00460

Verteporfin 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
ARPE-19 ~0.1 μg/ml cytotoxicity assay shows a dose-dependent toxicity 16987905
ARPE-19 0.01 μg/ml Function assay increases VEGF and reduces PEDF expression 16987905
ARPE-19 0.5 µg/ml cytotoxicity assay decreases viability by 55.5% 23441114
BxPC-3 10 μM Growth inhibitory assay inhibits cell proliferation completely 24069069

Verteporfin 动物研究

Dose Mice: 2 mg/kg - 6 mg/kg[1] (i.p.), 10 mg/kg[2] (i.p.), 100 mg/kg[3] (i.p.)
Rat: 0.25 mg/kg - 1 mg/kg[4] (i.v.)
Cynomolgus monkey: 0.25 mg/kg - 1 mg/kg[5] (i.v.)
Administration i.p., i.v.
Pharmacokinetics
Animal Rats[6]
Dose 2 mg/kg
Administration i.v.
AUC0-inf 13.653 μg·h/ml (male)
12.628 μg·h/ml (female)
T1/2 7.12 h (male)
2.94 h (female)
Tmax 0.017 h (male)
0.017 h (female)
CL 2.44 ml/min/kg (male)
2.64 ml/min/kg (female)
Cmax 20.360 μg/ml (male)
25.203 μg/ml (female)
Vss 0.57 L/kg (male)
0.35 L/kg (female)
AUC0→t 9.297 μg·h/ml (male)
11.323 μg·h/ml (female)

Verteporfin 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00211484 Age-Related Macular Degenerati... 展开 >>ons. Subfoveal Neovascularization. 收起 << Phase 2 Completed - United States, New York ... 展开 >> Manhattan Eye, Ear & Throat Hospital New York, New York, United States, 10021 收起 <<
NCT02587767 Acute Central Serous Chorioret... 展开 >>inopathy 收起 << Not Applicable Active, not recruiting December 2018 China, Guangdong ... 展开 >> Zhongshan Ophthalmic Center, Sun Yat-sen University Guangzhou, Guangdong, China, 510060 收起 <<
NCT02072408 Polypoidal Choroidal Vasculopa... 展开 >>thy Without Active Polyp 收起 << Phase 4 Completed - Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Seongnam, Gyunggi-do, Korea, Republic of Konyang University Kim's Eye Hospital Seoul, Korea, Republic of Samsung Medical Center Seoul, Korea, Republic of 收起 <<

Verteporfin 参考文献

[1]Morishita T, et al. The photosensitizer verteporfin has light-independent anti-leukemic activity for Ph-positive acute lymphoblastic leukemia and synergistically works with BMS-354825. Oncotarget. 2016 Aug 2.

[2]Pan W, et al. Verteporfin can Reverse the NSC 125973 Resistance Induced by YAP Over-Expression in HCT-8/T Cells without Photoactivation through Inhibiting YAP Expression. Cell Physiol Biochem. 2016;39(2):481-90.

[3]Donohue E, et al. The autophagy inhibitor verteporfin moderately enhances the antitumor activity of gemcitabine in a pancreatic ductal adenocarcinoma model.J Cancer. 2013 Aug 28;4(7):585-96.

Verteporfin 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.39mL

0.28mL

0.14mL

6.96mL

1.39mL

0.70mL

13.91mL

2.78mL

1.39mL

Verteporfin 技术信息

CAS号129497-78-5
分子式
分子量
别名 CL 318952;BPD-MA;DB00460, CL 318952, BPD-MA, BpdMA, Benzoporphyrin D, Benzoporphyrin derivative monoacid ring A, Verteporfin, Visudyne.
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

DMF: 10 mg/mL，配合低频超声，并水浴加热至45℃助溶
动物实验配方

Tags: Verteporfin | 129497-78-5 | CL 318952 | CL318952 | CL-318952 | YAP Inhibitor | Stem Cell/Wnt | Apoptosis | Autophagy | YAP | Apoptosis | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Verteporfin 纯度/质量文件 | Verteporfin 亚型比较 | Verteporfin 生物活性 | Verteporfin 细胞研究 | Verteporfin 动物研究 | Verteporfin 临床数据 | Verteporfin 参考文献 | Verteporfin 实验方案 | Verteporfin 技术信息

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