Verteporfin

别名: CL 318952 中文名称:维替泊芬

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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

Verteporfin Chemical Structure

CAS: 129497-78-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) 2760.03 现货
10mg 2607.44 现货
50mg 7928.11 现货
100mg 13677.3 现货
1g 81818.1 现货
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Verteporfin相关产品

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
VDA [1]
(Endothelial cells)
YAP/TEAD interaction [3]
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]

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

体外溶解度
批次:

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
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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