Verteporfin
别名: CL 318952 中文名称：维替泊芬
此产品请避光密封保存。
Verteporfin是一种能够抑制YAP-TEAD相互作用的小分子化合物，抑制YAP诱导的肝脏过度生长。同时，它还是一种有效的衍生自卟啉的第二代光敏剂。Verteporfin 是一种自噬抑制剂。Verteporfin 可抑制细胞增殖并诱导凋亡。
Verteporfin Chemical Structure
CAS: 129497-78-5
产品质控
批次：
纯度：
99.59%
99.59
Verteporfin相关产品
| 相关产品 | Vadimezan (DMXAA) Plinabulin | 点击展开 |
|---|---|---|
| 相关化合物库 | 酪氨酸激酶抑制剂分子库 PI3K/Akt 抑制剂库 血管生成相关化合物库 HIF-1信号通路化合物库 FDA抗癌药物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| Antitumor assay | B16F10 | 2 mg/kg | 2 hrs | Antitumor activity against B16F10 cells implanted in C57BL/6 mouse assessed as tumor growth inhibition at 2 mg/kg, iv administered for 2 hrs followed by irradiation with laser at 150 J/cm'2 for 10 mins | 27136389 |
| RB383 | Growth inhibitory assay | ~1 μg/ml | decreases retinoblastoma cell proliferation | 18579764 | |
| RB355 | Growth inhibitory assay | ~1 μg/ml | decreases retinoblastoma cell proliferation | 18579764 | |
| RB247C3 | Growth inhibitory assay | ~1 μg/ml | decreases retinoblastoma cell proliferation | 18579764 | |
| WERI-Rb1 | Growth inhibitory assay | ~1 μg/ml | decreases retinoblastoma cell proliferation | 18579764 | |
| Y-79 | Growth inhibitory assay | ~1 μg/ml | decreases retinoblastoma cell proliferation | 18579764 | |
| ARPE-19 | Function assay | 0.01 μg/ml | increases VEGF and reduces PEDF expression | 16987905 | |
| ARPE-19 | cytotoxicity assay | ~0.1 μg/ml | shows a dose-dependent toxicity | 16987905 | |
| SVEC4-10 | Function assay | 200 ng/ml | induces stress actin fiber formation | 16467106 | |
| SVEC4-10 | Function assay | 200 ng/ml | induces microtubule depolymerization | 16467106 | |
| RIF-1 | cytotoxicity assay | 1 μg/ml | decrease to 20 ± 5% cell survival | 12615718 | |
| RIF-1 | Function assay | 1 μg/ml | decreases oxygen consumption | 12615718 | |
| Jurkat | Apoptosis assay | ~280 nM | induces a Bcl-2-dependent apoptosis | 11245415 | |
| HL-60 | cytotoxicity assay | ~100 ng/mL | inhibits cell viability | 10607710 | |
| HL-60 | Function assay | ~100 ng/mL | increases DNA fragmentation levels | 10607710 | |
| hFibro | cytotoxicity assay | 0.5 µg/ml | decreases viability by 86,5% | 23441114 | |
| pTMC | cytotoxicity assay | 0.5 µg/ml | decreases viability by 92.9% | 23441114 | |
| hTMC | cytotoxicity assay | 0.5 µg/ml | decreases viability by 88.9% | 23441114 | |
| ARPE-19 | cytotoxicity assay | 0.5 µg/ml | decreases viability by 55.5% | 23441114 | |
| Panc-1 | Growth inhibitory assay | 10 μM | inhibits cell proliferation | 24069069 | |
| MIA PaCa-2 | Growth inhibitory assay | 10 μM | inhibits cell proliferation | 24069069 | |
| BxPC-3 | Growth inhibitory assay | 10 μM | inhibits cell proliferation completely | 24069069 | |
| SU86.86 | Growth inhibitory assay | 10 μM | inhibits cell proliferation completely | 24069069 | |
| MCF-7 | Autophagy assay | 10 μM | inhibits gemcitabine-induced autophagy | 24069069 | |
| WERI | Growth inhibitory assay | ~10 μg/ml | inhibits growth of retinoblastoma cells | 24837142 | |
| WERI | Function assay | ~10 μg/ml | blocks cell cycle progression | 24837142 | |
| Y-79 | Function assay | ~10 μg/ml | blocks cell cycle progression | 24837142 | |
| Y-79 | Function assay | ~10 μg/ml | affects YAP-TEAD proto-oncogene pathway | 24837142 | |
| Y-79 | Function assay | ~10 μg/ml | down-regulates pluripotency marker OCT-4 | 24837142 | |
| Phototoxicity assay | B16F10 | 24 hrs | IC50 = 1.07 μM | 27136389 | |
| Phototoxicity assay | B16F10 | 24 hrs | IC50 = 1.2 μM | 27136389 | |
| Phototoxicity assay | A375 | 24 hrs | IC50 = 2.06 μM | 27136389 | |
| Dark toxicity assay | B16F10 | 48 hrs | IC50 = 24.92 μM | 27136389 | |
| Dark toxicity assay | B16F10 | 48 hrs | IC50 = 25.03 μM | 27136389 | |
| Dark toxicity assay | A375 | 48 hrs | IC50 = 36.33 μM | 27136389 | |
| qHTS assay | TC32 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| qHTS assay | U-2 OS | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| qHTS assay | A673 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| qHTS assay | DAOY | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| qHTS assay | Saos-2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| qHTS assay | BT-37 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| qHTS assay | RD | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| qHTS assay | SK-N-SH | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| qHTS assay | BT-12 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| qHTS assay | MG 63 (6-TG R) | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| qHTS assay | OHS-50 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| qHTS assay | Rh41 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| qHTS assay | SJ-GBM2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| qHTS assay | SK-N-MC | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| qHTS assay | LAN-5 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Verteporfin是一种能够抑制YAP-TEAD相互作用的小分子化合物，抑制YAP诱导的肝脏过度生长。同时，它还是一种有效的衍生自卟啉的第二代光敏剂。Verteporfin 是一种自噬抑制剂。Verteporfin 可抑制细胞增殖并诱导凋亡。 | ||
|---|---|---|---|
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | 对于穿透组织最好的波长(i.e.，大约700 nm)下的吸收光，Verteporfin比hematoporphyrin大约有效4倍，从而比hematoporphyrin提供了更高的细胞毒性(在人贴壁细胞中10倍以上)。Verteporfin是亲脂性的，与正常细胞或静息细胞相比，更容易被恶性的或激活的细胞摄取。Verteporfin与LDL结合形成一个复合物，随后可能通过LDL受体或者內吞作用被增殖细胞 (例如，新生血管内皮细胞) 摄取。Verteporfin疗法通过血管通道中形成血栓实现新生血管区的血管造影完全闭塞，进而引起选择性血管内皮损伤。Verteporfin疗法选择性诱导可再生的和离体的脉络膜毛细血管闭塞，而不改变覆盖的光感受器或神经节细胞，如光学和电子显微镜所示。[1] HL-60细胞中胱天蛋白酶-3和胱天蛋白酶-9的活化以及PARP的裂解映射出，光存在下，Verteporfin快速使细胞凋亡改变，该改变会被普通半胱天冬酶抑制剂ZVAD.fmk阻断。[2] |
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|---|---|---|---|---|
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | ECAD / Vimentin / Sox2 / CD44 / CD133 c-Myc / Bcl-2 p-S6(S240/244) / p-4EBP1(S65) beta-catenin |
|
30467925 | |
| Growth inhibition assay | Cell viability |
|
28042502 | |
| Immunofluorescence | p-YAP(Y357) Calreticulin YAP1 |
|
28404908 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Verteporfin可用于脉络膜血管和CNV的血管可视化，这表明光敏剂在猴子的实验性CNV中快速集聚。Verteporfin在建立的兔子眼睛的脉络膜脉管系统，RPE，以及光感受器中迅速积累。在小鼠体内，静脉注射3小时后，Verteporfin达到最大组织水平，随后在24小时内迅速下降。Verteporfin在体内代谢为活性较低的形式，并且迅速清除，主要通过粪便排泄，一小部分通过尿液排泄。Verteporfin疗法有效的选择性阻止了荧光染料从实验性诱导的猴子CNV的泄漏。[1] |
|
|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT04590664 | Recruiting | Glioblastoma|Recurrent Glioblastoma |
Emory University|National Cancer Institute (NCI) |
January 15 2021 | Phase 1|Phase 2 |
| NCT03797547 | Unknown status | Myopic Choroidal Neovascularisation |
Poitiers University Hospital |
June 22 2018 | -- |
| NCT01846273 | Completed | Age-related Macular Degeneration|Polypoidal Choroidal Vasculopathy |
Novartis Pharmaceuticals|Novartis |
August 7 2013 | Phase 4 |
| NCT00423189 | Terminated | Age-Related Macular Degeneration |
David M. Brown M.D.|Novartis Pharmaceuticals|Greater Houston Retina Research |
January 2007 | Phase 4 |
| NCT00403442 | Terminated | Macular Degeneration |
Vitreous -Retina- Macula Consultants of New York|QLT Inc. |
September 2006 | Phase 1 |
化学信息&溶解度
| 分子量 | 718.79 | 分子式 | C41H42N4O8 |
| CAS号 | 129497-78-5 | SDF | Download Verteporfin SDF |
| Smiles | COC(=O)CCC1=C(C)C2=CC3=NC(=CC4=C(C)C(=C([NH]4)C=C5N=C(C=C1[NH]2)C(=C5C)CCC(O)=O)C=C)C6=CC=C(C(C(=O)OC)C36C)C(=O)OC | ||
| 储存条件(自收到货起) | 3年 -20°C(避光) 粉状 | ||
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体外溶解度 |
DMSO : 100 mg/mL ( (139.12 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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