Verteporfin

目录号:S1786 别名: CL 318952

Verteporfin  Chemical Structure

Molecular Weight(MW): 718.79

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。

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客户使用Selleck该产品发表文献22篇:

产品安全说明书

VDA抑制剂选择性比较

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。
靶点
VDA [1]
(Endothelial cells)
YAP/TEAD interaction [3]
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL-60 NFfCWZVHfW6ldHnvckBie3OjeR?= NHnZUGF,OTByIH7nM41N M3;SZ2ROW09? NE\5fphqdmO{ZXHz[ZMhTE6DIH\yZYdu\W62YYTpc44hdGW4ZXzz M1LFNVExPjB5N{Gw
HL-60 NH3KeoNkgXSxdH;4bYNqfHliYYPzZZk> M3O2Zp4yODBibnevcWw> MnfCSG1UVw>? NVHZbFB5cW6qaXLpeJMh[2WubDD2bYFjcWyrdIm= NF;zR4wyODZyN{exNC=>
Jurkat MYnBdI9xfG:|aYOgZZN{[Xl? M{fKfZ4zQDBibl2= MWDEUXNQ NGfu[3VqdmS3Y3XzJIEhSmOuLUKt[IVx\W6mZX70JIFxd3C2b4Ppdy=> NVzlcJJlOTF{NEW0NVU>
RIF-1 M4e5bGZ2dmO2aX;uJIF{e2G7 NFfrW5EyKM7:Zz;tcC=> NHvs[2ZFVVOR M{fEcoRm[3KnYYPld{BwgHmpZX6gZ49ve3WvcITpc44> MnfENVI3OTV5MUi=
RIF-1 MnSzZ5l1d3SxeHnjbZR6KGG|c3H5 NEDId4syKM7:Zz;tcC=> NIrEfFBFVVOR Mk\t[IVkemWjc3WgeI8hOjBiwsGgOUUh[2WubDDzeZJ3cX[jbB?= MYKxNlYyPTdzOB?=
SVEC4-10 MoDWSpVv[3Srb36gZZN{[Xl? NEG0[JEzODBibnevcYw> M{jXfmROW09? NG\nOotqdmS3Y3XzJI1q[3KxdIXieYxmKGSncH;sfY1memm8YYTpc44> NX\DTlV3OTZ2NkexNFY>
SVEC4-10 MYDGeY5kfGmxbjDhd5NigQ>? MWSyNFAhdmdxbXy= MVPEUXNQ NIm1UWNqdmS3Y3XzJJN1emW|czDhZ5RqdiCoaXLldkBnd3KvYYTpc44> M1nYdVE3PDZ5MUC2
ARPE-19 M2LpPYN6fG:2b4jpZ4l1gSCjc4PhfS=> NHL0ToZ,OC5zIN88[{9udA>? NHnqWHZFVVOR NWj4UXpRe2ixd4OgZUBld3OnLXTldIVv\GWwdDD0c5hq[2m2eR?= MnfGNVY6QDd7MEW=
ARPE-19 MnvnSpVv[3Srb36gZZN{[Xl? MX:wMlAyKM7:Zz;tcC=> NVj2VlJZTE2VTx?= NIX5VWxqdmO{ZXHz[ZMhXkWJRjDhcoQhemWmdXPld{BRTUSIIHX4dJJme3Orb36= NFXvNnQyPjl6N{mwOS=>
Y-79 Mk\QS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUD+NUDPxGdxbXy= NWnLWINjTE2VTx?= M2WzWIRm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= MXqxPFU4QTd4NB?=
WERI-Rb1 M4n0Vmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MnPBglEh|rypL33s M1XrOWROW09? NF72XlJl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u NUnhRWlNOTh3N{m3OlQ>
RB247C3 NIn6Xm9Iem:5dHigbY5pcWKrdH;yfUBie3OjeR?= M3\jO54yKM7:Zz;tcC=> NHzHUVZFVVOR M3X5Z4Rm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= NVHv[FNtOTh3N{m3OlQ>
RB355 Mm[4S5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M3XwZZ4yKM7:Zz;tcC=> M2PtNWROW09? Mn;u[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= NXvIVYw1OTh3N{m3OlQ>
RB383 NHjQfmVIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NUnvR5NjhjFizsznM41t M2PaTWROW09? NEDTUZBl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u MUSxPFU4QTd4NB?=
hFibro MWjjfZRwfG:6aXPpeJkh[XO|YYm= NH\EeYIxNjViwsXnM41t MY\EUXNQ Mkno[IVkemWjc3XzJJZq[WKrbHn0fUBjgSB6Njy1KS=> MkPBNlM1PDFzMUS=
pTMC NXHFb4w6[3m2b4TvfIlkcXS7IHHzd4F6 NXnlVGNqOC53INM1[{9udA>? NH;tS29FVVOR MX3k[YNz\WG|ZYOgeoli[mmuaYT5JIJ6KDl{Lkml NYX2NodXOjN2NEGxNVQ>
hTMC NHrINWhkgXSxdH;4bYNqfHliYYPzZZk> NXTlcYhuOC53INM1[{9udA>? MljYSG1UVw>? NWjIbnFT\GWlcnXhd4V{KH[rYXLpcIl1gSCkeTC4PE46LQ>? NIPuR4wzOzR2MUGxOC=>
ARPE-19 M2rRO4N6fG:2b4jpZ4l1gSCjc4PhfS=> NXrDfJl{OC53INM1[{9udA>? Mmn5SG1UVw>? NF7VW|dl\WO{ZXHz[ZMhfmmjYnnsbZR6KGK7IEW1MlUm MX2yN|Q1OTFzNB?=
Panc-1 M{nGOWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Mmq1NVAh|ryP NIDIfHpFVVOR Mmi4bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u NXTud5M1OjRyNkmwOlk>
MIA PaCa-2 MlPVS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVHNV2FvOTBizszN M4fNeWROW09? MYfpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36= NXntT45{OjRyNkmwOlk>
BxPC-3 M3znOGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NG\ITlEyOCEQvF2= NUjZWoI2TE2VTx?= Mmn1bY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJINwdXCuZYTlcJk> NF3LdFUzPDB4OUC2PS=>
SU86.86 NWXmW2VkT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGrHNZIyOCEQvF2= MVLEUXNQ NYPtdI03cW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9vKGOxbYDs[ZRmdHl? NUTNb5pMOjRyNkmwOlk>
MCF-7 NFznd4tCfXSxcHjh[5kh[XO|YYm= NXjhSXJ6OTBizszN MYDEUXNQ MVfpcohq[mm2czDn[Y1kcXSjYnnu[U1qdmS3Y3XkJIF2fG:yaHHnfS=> MmnWNlQxPjlyNkm=
WERI NX7XZWF2T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M2nWNZ4yOCEQvHevcYw> NHTTZ4lFVVOR NXzIbWtDcW6qaXLpeJMh\3Kxd4ToJI9nKHKndHnuc4Jt[XO2b33hJINmdGy| NIPBPJgzPDh|N{G0Ni=>
WERI MUXGeY5kfGmxbjDhd5NigQ>? NWjZOZJ[hjFyIN88[{9udA>? M3zqU2ROW09? MWDicI9kc3NiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> MYSyOFg{PzF2Mh?=
Y-79 MlXHSpVv[3Srb36gZZN{[Xl? NVi4bo9mhjFyIN88[{9udA>? MVrEUXNQ NXTJe|JE[myxY3vzJINmdGxiY4njcIUheHKxZ4Lld5Nqd25? M1rZWVI1QDN5MUSy
Y-79 MWrGeY5kfGmxbjDhd5NigQ>? M4L0bp4yOCEQvHevcYw> MXPEUXNQ M2XDeYFn\mWldIOgXWFRNVSHQVSgdJJwfG9vb37jc4dmdmVicHH0bJdigQ>? MmS0NlQ5OzdzNEK=
Y-79 MnjwSpVv[3Srb36gZZN{[Xl? MVr+NVAh|rypL33s NHHaN|JFVVOR MkT3[I94di2{ZXf1cIF1\XNicHz1dolxd3SnbnP5JI1iemuncjDPR3QuPA>? NILIOWIzPDh|N{G0Ni=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-S6(S240/244) / p-4EBP1(S65); 

PubMed: 28202507     


KLE, EFE184 and NOU-1 were treated with Verteporfin (0.1 μM, 0.3 μM). After 36h, cell lysates were western blotted with indicated antibodies. Bands are from one of three independent experiments.

c-Myc / Bcl-2; 

PubMed: 29416644     


In CAL27 cell lines, the expression of BCL-2 and C-MYC proteins decreased with the increase of Verteporfin concentration. The presented columns are given as the means ± SD. *p < 0.05, **P < 0.01, ***p < 0.001.

ECAD / Vimentin / Sox2 / CD44 / CD133; 

PubMed: 30467925     


Yes-associated protein 1 (YAP1), E-cadherin, vimentin (epithelial-mesenchymal transition [EMT] pathway), SOX2 CD44 and CD133 (autophagy markers) were detected by western blot in control, verteporfin (1 μmol/L) and verteporfin + 231-taxol (0.5 μmol/L) resistance groups.

beta-catenin; 

PubMed: 28202507     


KLE, EFE184, NOU-1 and SKUT-2 were treated with 3 μM Verteporfin. After 24h, cell lysates were western blotted with indicated antibodies. Bands are from one of three independent experiments.

28202507 29416644 30467925
Growth inhibition assay
Cell viability; 

PubMed: 28042502     


A: Cell viability was determined by MTS assay after the UM cells were exposed to verteporfin for 72 hours. B: After treated with various concentrations of verteporfin for 24 hours, the UM cells (e.g., 92.1, Mel 270, Omm 1, Omm 2.3) were seeded in drug-free soft agar culture for 14 days. Colonies were counted. 

28042502
Immunofluorescence
YAP1; 

PubMed: 30254296     


Treatment of U343 cells with 5 μM VP between 1-8 h in both 21% and 1% O2 induced morphological changes. Scale bar represents 10 µm. VP: Verteporfin

Calreticulin; 

PubMed: 30254296     


Calreticulin (CRT) significantly increased in VP-treated (5 µM, 2 h) U87 cells in both 21% and 1% O2 indicating likely ER stress.

p-YAP(Y357); 

PubMed: 28404908     


Confocal images of HEC-1-B cells and organoids which were subjected to immunofluorescence detection of A. YAP and B. phospho-YAP after VP treatment. YAP and phospho-YAP are conjugated with goat anti-mouse and goat anti-rabbit Alexa flour secondary antibodies respectively. (A) Upper panel bar=63x and lower panel bar = 20x. (B) Upper panel bar=63x and lower panel bar = 20x.

30254296 28404908
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

溶解度 (25°C)

体外 DMSO 100 mg/mL (139.12 mM)
Water Insoluble
Ethanol Insoluble

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 718.79
化学式

C41H42N4O8

CAS号 129497-78-5
储存条件 powder
in solvent
别名 CL 318952

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、MSDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03067051 Recruiting Recurrent Prostate Cancer SpectraCure AB March 21 2017 Phase 1
NCT03067051 Recruiting Recurrent Prostate Cancer SpectraCure AB March 21 2017 Phase 1
NCT03033225 Recruiting Pancreatic Cancer Non-Resectable Mayo Clinic January 5 2017 Phase 2
NCT03033225 Recruiting Pancreatic Cancer Non-Resectable Mayo Clinic January 5 2017 Phase 2
NCT02939274 Recruiting Metastatic Breast Cancer Rogers Sciences Inc. October 2016 Phase 2
NCT02939274 Recruiting Metastatic Breast Cancer Rogers Sciences Inc. October 2016 Phase 2

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VDA Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID