Verteporfin

Catalog No.S1786 Synonyms: CL 318952

Verteporfin  Chemical Structure

Molecular Weight(MW): 718.79

Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin.

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6 Customer Reviews

  • Verteporfin treatment inhibits proliferation and induces apoptosis of Tsc1-null cells in vivo. Mice were administered i.p. with vehicle or verteporfin at a dose of 100 mg/kg every other day for 10 d before sacrifice. Mice were sacrificed at 6 wk of age. Three independent experiments were performed and mice in different treatments were pooled for analysis. Percentage of Ki67 and αSMA double-positive cells in α-SMA+ mesenchymal lesions in the indicated kidneys. Immunofluorescence staining and counting were performed on three sagittal sections from different kidney regions for each mouse.

    J Exp Med 2014 211(11), 2249-63. Verteporfin purchased from Selleck.

    A representative immunostaining results of p-EGFR, p-ERK, YAP1, and cleavage caspase-3 in tumors of each group of nude mice.

    Theranostics, 2017, 7(5):1114-1132. Verteporfin purchased from Selleck.

  • Colony formation in H520 cells and H1581 cells that were with or without verteporfin

    Cancer Lett, 2018, 423:36-46. Verteporfin purchased from Selleck.

    The effects of ADR and Verteporfin on the growth of HCC xenograft derived from MHCC-97H cells (n = 5 for each group). Representative images of IHC staining of KI67 and cleaved caspase-3 in tumors. Scale bar: 100 μm.

    EBioMedicine, 2018, 35:142-154. Verteporfin purchased from Selleck.

  • The indicated cell lines were treated with control (Ctrl) or YAP-targeting siRNAs and growth assessed by XTT proliferation assays at the indicated time points. The mean and +SD are shown for three independent experiments. (Left panel, *, P < 0.05, significantly different from U87Rictor DMSO; Right panel, *, P < 0.05, significantly different from H4Rictor DMSO).

    J Biol Chem, 2015, 290(32): 19387-401 . Verteporfin purchased from Selleck.

    The levels of YAP, phospho-YAP (S127), and its downstream targeted molecules CTGF and CYR61 were analyzed by Western blotting after UM cells were exposed to verteporfin for 24 hours.

    Am J Cancer Res, 2016, 6(12):2816-2830.. Verteporfin purchased from Selleck.

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Biological Activity

Description Verteporfin is a small molecule that inhibits TEAD–YAP association and YAP-induced liver overgrowth. It is also a potent second-generation photosensitizing agent derived from porphyrin.
Targets
VDA [1]
(Endothelial cells)
YAP/TEAD interaction [3]
In vitro

Verteporfin is about four times more efficient in absorbing light at wavelengths that penetrate tissues best (i.e., around 700 nm) and thus provides a much higher cytotoxic effect than hematoporphyrin (10 times more in human adherent cell lines). Verteporfin is lipophilic and is more readily taken up by malignant or activated cells, compared with normal or resting cells. Verteporfin binds with LDL to form a complex, which is then taken up into proliferating cells (e.g., neovascular endothelial cells) probably via LDL receptors and endocytosis. Verteporfin therapy achieves complete angiographic occlusion of the neovascular compartment by thrombosis of vascular channels, following selective endothelial damage. Verteporfin therapy selectively induces reproducible and isolated choriocapillary occlusion without alteration of overlying photoreceptors or ganglion cells, as shown by light and electron microscopy. [1] Verteporfin conbined with light rapidly exhibits apoptotic changes reflected by caspase-3 and caspase-9 activation and PARP cleavage in HL-60 cells, changes that are blocked by the general caspase inhibitor ZVAD.fmk. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HL-60 Ml\ESpVv[3Srb36gZZN{[Xl? NGnMTXF,OTByIH7nM41N M3;0eWROW09? M1Lo[4lv[3KnYYPld{BFVkFiZoLh[41mdnSjdHnvckBt\X[nbIO= MWSxNFYxPzdzMB?=
HL-60 NWnpT2Zs[3m2b4TvfIlkcXS7IHHzd4F6 MWX+NVAxKG6pL33M M3r5ZmROW09? MVvpcohq[mm2czDj[YxtKH[rYXLpcIl1gQ>? Mnm3NVA3ODd5MUC=
Jurkat Mn7URZBweHSxc3nzJIF{e2G7 M33RUp4zQDBibl2= MXvEUXNQ NFPh[WtqdmS3Y3XzJIEhSmOuLUKt[IVx\W6mZX70JIFxd3C2b4Ppdy=> MkH6NVEzPDV2MUW=
RIF-1 NF;VTolHfW6ldHnvckBie3OjeR?= MmX2NUDPxGdxbXy= NFrs[FdFVVOR NHW5UHJl\WO{ZXHz[ZMhd3i7Z3XuJINwdnO3bYD0bY9v MnfoNVI3OTV5MUi=
RIF-1 M4PYeYN6fG:2b4jpZ4l1gSCjc4PhfS=> MofxNUDPxGdxbXy= MmPSSG1UVw>? NWTVVHZ3\GWlcnXhd4UhfG9iMkCgxtEhPSViY3XscEB{fXK4aY\hcC=> Ml\ONVI3OTV5MUi=
SVEC4-10 MlvwSpVv[3Srb36gZZN{[Xl? MVeyNFAhdmdxbXy= MkX0SG1UVw>? MlnZbY5lfWOnczDtbYNzd3S3YoXs[UBl\XCxbInt[ZJqgmG2aX;u MWOxOlQ3PzFyNh?=
SVEC4-10 MWLGeY5kfGmxbjDhd5NigQ>? NHG0UYwzODBibnevcYw> M{fZTWROW09? NFW1eJpqdmS3Y3XzJJN1emW|czDhZ5RqdiCoaXLldkBnd3KvYYTpc44> Mmn6NVY1PjdzME[=
ARPE-19 MWPjfZRwfG:6aXPpeJkh[XO|YYm= MlKxglAvOSEQvHevcYw> NUPVcmo3TE2VTx?= NIHteGJ{cG:5czDhJIRwe2VvZHXw[Y5l\W62IITvfIlkcXS7 NIrIWnEyPjl6N{mwOS=>
ARPE-19 M2P2[GZ2dmO2aX;uJIF{e2G7 M{jIO|AvODFizsznM41t MmHRSG1UVw>? M1n6dYlv[3KnYYPld{BXTUeIIHHu[EBz\WS3Y3XzJHBGTEZiZYjwdoV{e2mxbh?= MVOxOlk5PzlyNR?=
Y-79 NGPzT|NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHTJWmZ,OSEQvHevcYw> NGDIPHlFVVOR MVXk[YNz\WG|ZYOgdoV1cW6xYnzhd5RwdWFiY3XscEBxem:uaX\ldoF1cW:w NHi1XYgyQDV5OUe2OC=>
WERI-Rb1 NHLhV3VIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NWPWPI5UhjFizsznM41t MnfrSG1UVw>? M1zWR4Rm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= MkezNVg2Pzl5NkS=
RB247C3 MkLkS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NVvLRmpXhjFizsznM41t M3P3WWROW09? MkDm[IVkemWjc3XzJJJmfGmwb3LsZZN1d22jIHPlcIwheHKxbHnm[ZJifGmxbh?= M2DQU|E5PTd7N{[0
RB355 NUjQU5VPT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3zXWp4yKM7:Zz;tcC=> M{nXWWROW09? M{DkbYRm[3KnYYPld{Bz\XSrbn;icIF{fG:vYTDj[YxtKHC{b3zp[oVz[XSrb36= NWfQcW1VOTh3N{m3OlQ>
RB383 MknGS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NHnmNpd,OSEQvHevcYw> M2OwW2ROW09? NGXZXJRl\WO{ZXHz[ZMhemW2aX7vZoxie3SxbXGgZ4VtdCCycn;sbYZmemG2aX;u MXKxPFU4QTd4NB?=
hFibro MnvkZ5l1d3SxeHnjbZR6KGG|c3H5 MkPHNE42KML3Zz;tcC=> MYfEUXNQ NXrGTGdl\GWlcnXhd4V{KH[rYXLpcIl1gSCkeTC4Okw2LQ>? MoTINlM1PDFzMUS=
pTMC M33JVYN6fG:2b4jpZ4l1gSCjc4PhfS=> MoC0NE42KML3Zz;tcC=> MYHEUXNQ NWXjWZlL\GWlcnXhd4V{KH[rYXLpcIl1gSCkeTC5Nk46LQ>? NX;BS2ROOjN2NEGxNVQ>
hTMC M{XVV4N6fG:2b4jpZ4l1gSCjc4PhfS=> MX[wMlUhyrWpL33s MlvySG1UVw>? M3n2XoRm[3KnYYPld{B3cWGkaXzpeJkh[nliOEiuPUU> NUOx[3NMOjN2NEGxNVQ>
ARPE-19 NUOyPVdC[3m2b4TvfIlkcXS7IHHzd4F6 M2q3[lAvPSEEtXevcYw> NXK4dZRZTE2VTx?= MnO1[IVkemWjc3XzJJZq[WKrbHn0fUBjgSB3NT61KS=> NXPTT297OjN2NEGxNVQ>
Panc-1 MmrrS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? M4r1dlExKM7:TR?= MXrEUXNQ MlPibY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;u MnnvNlQxPjlyNkm=
MIA PaCa-2 MXzHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MV2xNEDPxE1? MXHEUXNQ NWXvRXRzcW6qaXLpeJMh[2WubDDwdo9tcW[ncnH0bY9v NY[2V2tDOjRyNkmwOlk>
BxPC-3 Ml\VS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? Mmi0NVAh|ryP NYfyfJlGTE2VTx?= MmfubY5pcWKrdIOgZ4VtdCCycn;sbYZmemG2aX;uJINwdXCuZYTlcJk> MmDwNlQxPjlyNkm=
SU86.86 M1;DZWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NXH1bYhFOTBizszN MlXZSG1UVw>? MYPpcohq[mm2czDj[YxtKHC{b3zp[oVz[XSrb36gZ49ueGyndHXsfS=> NHnlOFEzPDB4OUC2PS=>
MCF-7 NUXve4VlSXW2b4DoZYd6KGG|c3H5 NWPacIhxOTBizszN M2rab2ROW09? NFjlc2JqdmirYnn0d{Bo\W2laYThZolv\S2rbnT1Z4VlKGG3dH;wbIFogQ>? MoLaNlQxPjlyNkm=
WERI MnnoS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NFP2ZWd,OTBizsznM41t MVLEUXNQ MWDpcohq[mm2czDndo94fGhib3[gdoV1cW6xYnzhd5RwdWFiY3XscJM> MW[yOFg{PzF2Mh?=
WERI NGXQbHBHfW6ldHnvckBie3OjeR?= NX;1fWxOhjFyIN88[{9udA>? M3zNfGROW09? MVXicI9kc3NiY3XscEBkgWOuZTDwdo9oemW|c3nvci=> NHu5PXIzPDh|N{G0Ni=>
Y-79 MXjGeY5kfGmxbjDhd5NigQ>? NEfYXlF,OTBizsznM41t NFTFZ2RFVVOR M1rRXoJtd2OtczDj[YxtKGO7Y3zlJJBzd2e{ZYPzbY9v MX6yOFg{PzF2Mh?=
Y-79 NIf6PWVHfW6ldHnvckBie3OjeR?= MXL+NVAh|rypL33s MmL2SG1UVw>? NIjrRY9i\m[nY4TzJHlCWC2WRVHEJJBzd3SxLX;uZ49o\W6nIIDheIh4[Xl? M3TZZlI1QDN5MUSy
Y-79 NEXPPVlHfW6ldHnvckBie3OjeR?= NGT6[IN,OTBizsznM41t MlPnSG1UVw>? M{DOR4Rwf25vcnXneYxifGW|IIDseZJqeG:2ZX7jfUBu[XKtZYKgU2NVNTR? MUKyOFg{PzF2Mh?=

... Click to View More Cell Line Experimental Data

In vivo Verteporfin can be used for angiographic visualization of choroidal vessels and CNV, which demonstrates that the photosensitizer accumulates rapidly in experimental CNV in monkeys. Verteporfin accumulates rapidly in the established vasculature of the choroid, RPE, and photoreceptors of rabbit eyes. Verteporfin reaches maximal tissue levels within 3 hours of intravenous injection, followed by a rapid decline within 24 hours in mice. Verteporfin is metabolized to a less active form in vivo and is cleared very rapidly, predominantly in the feces and a very small proportion excreted in urine. Verteporfin therapy effectively and selectively prevents fluorescein dye leakage from experimentally induced CNV in monkeys. [1]

Protocol

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 718.79
Formula

C41H42N4O8

CAS No. 129497-78-5
Storage powder
in solvent
Synonyms CL 318952

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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
NCT02939274 Recruiting Metastatic Breast Cancer Rogers Sciences Inc. October 2016 Phase 2
NCT02702700 Recruiting Pleural Effusion Malignant Centre Hospitalier Universitaire Vaudois January 2016 Phase 1
NCT02495181 Recruiting Polypoidal Choroidal Vasculopathy Association for Innovation and Biomedical Research on Light and Image|European Vision Institute Clinical Research Network January 2016 Phase 4
NCT02457026 Withdrawn Neovascular Age-related Macular Degeneration Duke University|Bausch & Lomb Incorporated January 2016 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID