Verteporfin

Catalog No.S1786 Batch:S178613

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Technical Data

Formula

C41H42N4O8

Molecular Weight 718.79 CAS No. 129497-78-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (139.12 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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. Verteporfin is an autophagy inhibitor. Verteporfin inhibits cell proliferation and induces apoptosis.
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]

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 (from reference)

Cell Assay:

[4]

  • Cell lines

    Ki67+ and Sox10+ cells

  • Concentrations

    2 uM

  • Incubation Time

    72 h

  • Method

    Cells were treated with verteporfin (2 µM) for 72 hr for Brdu staining.

Animal Study:

[4]

  • Animal Models

    Atoh1-Ptch mice

  • Dosages

    100 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by J Exp Med, 2014, 211(11), 2249-63]

Data from [Data independently produced by , , Theranostics, 2017, 7(5):1114-1132]

Data from [Data independently produced by , , Cancer Lett, 2018, 423:36-46]

Data from [Data independently produced by , , EBioMedicine, 2018, 35:142-154]

Selleck's Verteporfin has been cited by 138 publications

Piezo1 expression in chondrocytes controls endochondral ossification and osteoarthritis development [ Bone Res, 2024, 12(1):12] PubMed: 38395992
AXL signal mediates adaptive resistance to KRAS G12C inhibitors in KRAS G12C-mutant tumor cells [ Cancer Lett, 2024, 587:216692] PubMed: 38342232
YAP-mediated GPER signaling impedes proliferation and survival of prostate epithelium in benign prostatic hyperplasia [ iScience, 2024, 27(3):109125] PubMed: 38420594
VAV2 orchestrates the interplay between regenerative proliferation and ribogenesis in both keratinocytes and oral squamous cell carcinoma [ Sci Rep, 2024, 14(1):4060] PubMed: 38374399
M2 macrophages promote subconjunctival fibrosis through YAP/TAZ signalling [ Ann Med, 2024, 56(1):2313680] PubMed: 38335557
YAP1 expression is associated with survival and immunosuppression in small cell lung cancer [ Cell Death Dis, 2023, 14(9):636] PubMed: 37752152
HLF promotes ovarian cancer progression and chemoresistance via regulating Hippo signaling pathway [ Cell Death Dis, 2023, 14(9):606] PubMed: 37709768
HLF promotes ovarian cancer progression and chemoresistance via regulating Hippo signaling pathway [ Cell Death Dis, 2023, 10.1038/s41419-023-06076-5] PubMed: 37709768
YAP1 expression is associated with survival and immunosuppression in small cell lung cancer [ Cell Death Dis, 2023, 10.1038/s41419-023-06053-y] PubMed: 37752152
Neuronopathic Gaucher disease models reveal defects in cell growth promoted by Hippo pathway activation [ Commun Biol, 2023, 6(1):431] PubMed: 37076591

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.