货号:A138297
同义名:
CL 318952; BPD-MA
Verteporfin, a benzoporphyrin derivative monoacid ring A, inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent.
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产品名称 | Autophagy ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
SBI-0206965 |
+++
ULK1, IC50: 108 nM ULK2, IC50: 711 nM |
95% | |||||||||||||||||
Hydroxychloroquine sulfate | ✔ | 99% | |||||||||||||||||
Valproic acid sodium | ✔ | HDAC | 97% | ||||||||||||||||
PFK-015 |
++
PFKFB3, IC50: 207 nM |
99%+ | |||||||||||||||||
MRT68921 HCl |
++++
ULK1, IC50: 2.9 nM ULK2, IC50: 1.1 nM |
99%+ | |||||||||||||||||
ROC-325 | ✔ | 99%+ | |||||||||||||||||
Autophinib |
+++
Autophagy, IC50: 40 nM |
99% | |||||||||||||||||
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。 |
靶点 |
|
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]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活性说明 | 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 | |
Animal study | 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]. | ||||||||||||||||||||
Pharmacokinetics |
|
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 << |
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 |
CAS号 | 129497-78-5 |
分子式 | C41H42N4O8 |
分子量 | 718.79 |
SMILES Code | NONE |
MDL No. | MFCD28098202 |
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 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |