Name: Verteporfin
Brand: Selleck Chemicals
SKU: S1786
Availability: InStock
Rating: 5 (160 reviews)

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Quality Control

Batch: Purity: 99.31%

99.31

Related Targets	EGFR VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2
Other VDA Inhibitors	Vadimezan (DMXAA) Plinabulin

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HL-60	Function assay	~100 ng/mL		DMSO	increases DNA fragmentation levels	10607710
HL-60	cytotoxicity assay	~100 ng/mL		DMSO	inhibits cell viability	10607710
Jurkat	Apoptosis assay	~280 nM		DMSO	induces a Bcl-2-dependent apoptosis	11245415
RIF-1	Function assay	1 μg/ml		DMSO	decreases oxygen consumption	12615718
RIF-1	cytotoxicity assay	1 μg/ml		DMSO	decrease to 20 ± 5% cell survival	12615718
SVEC4-10	Function assay	200 ng/ml		DMSO	induces microtubule depolymerization	16467106
SVEC4-10	Function assay	200 ng/ml		DMSO	induces stress actin fiber formation	16467106
ARPE-19	cytotoxicity assay	~0.1 μg/ml		DMSO	shows a dose-dependent toxicity	16987905
ARPE-19	Function assay	0.01 μg/ml		DMSO	increases VEGF and reduces PEDF expression	16987905
Y-79	Growth inhibitory assay	~1 μg/ml		DMSO	decreases retinoblastoma cell proliferation	18579764
WERI-Rb1	Growth inhibitory assay	~1 μg/ml		DMSO	decreases retinoblastoma cell proliferation	18579764
RB247C3	Growth inhibitory assay	~1 μg/ml		DMSO	decreases retinoblastoma cell proliferation	18579764
RB355	Growth inhibitory assay	~1 μg/ml		DMSO	decreases retinoblastoma cell proliferation	18579764
RB383	Growth inhibitory assay	~1 μg/ml		DMSO	decreases retinoblastoma cell proliferation	18579764
hFibro	cytotoxicity assay	0.5 µg/ml		DMSO	decreases viability by 86,5%	23441114
pTMC	cytotoxicity assay	0.5 µg/ml		DMSO	decreases viability by 92.9%	23441114
hTMC	cytotoxicity assay	0.5 µg/ml		DMSO	decreases viability by 88.9%	23441114
ARPE-19	cytotoxicity assay	0.5 µg/ml		DMSO	decreases viability by 55.5%	23441114
Panc-1	Growth inhibitory assay	10 μM		DMSO	inhibits cell proliferation	24069069
MIA PaCa-2	Growth inhibitory assay	10 μM		DMSO	inhibits cell proliferation	24069069
BxPC-3	Growth inhibitory assay	10 μM		DMSO	inhibits cell proliferation completely	24069069
SU86.86	Growth inhibitory assay	10 μM		DMSO	inhibits cell proliferation completely	24069069
MCF-7	Autophagy assay	10 μM		DMSO	inhibits gemcitabine-induced autophagy	24069069
WERI	Growth inhibitory assay	~10 μg/ml		DMSO	inhibits growth of retinoblastoma cells	24837142
WERI	Function assay	~10 μg/ml		DMSO	blocks cell cycle progression	24837142
Y-79	Function assay	~10 μg/ml		DMSO	blocks cell cycle progression	24837142
Y-79	Function assay	~10 μg/ml		DMSO	affects YAP-TEAD proto-oncogene pathway	24837142
Y-79	Function assay	~10 μg/ml		DMSO	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
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (139.12 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.96mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	718.79	Formula	C₄₁H₄₂N₄O₈	Storage (From the date of receipt)	3 years-20°C （in the dark）powder
CAS No.	129497-78-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CL 318952			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

Mechanism of Action

Targets/IC₅₀/Ki	VDA (Endothelial cells) YAP/TEAD interaction
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). This compound is lipophilic and is more readily taken up by malignant or activated cells, compared with normal or resting cells. It 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. This therapy achieves complete angiographic occlusion of the neovascular compartment by thrombosis of vascular channels, following selective endothelial damage. It selectively induces reproducible and isolated choriocapillary occlusion without alteration of overlying photoreceptors or ganglion cells, as shown by light and electron microscopy. This chemical 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.
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. This compound accumulates rapidly in the established vasculature of the choroid, RPE, and photoreceptors of rabbit eyes. It reaches maximal tissue levels within 3 hours of intravenous injection, followed by a rapid decline within 24 hours in mice. This chemical 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. The therapy effectively and selectively prevents fluorescein dye leakage from experimentally induced CNV in monkeys.
References	[1] https://pubmed.ncbi.nlm.nih.gov/11094244/ [2] https://pubmed.ncbi.nlm.nih.gov/10607710/ [3] https://pubmed.ncbi.nlm.nih.gov/22677547/ [4] https://pubmed.ncbi.nlm.nih.gov/29438698/ [5] https://pubmed.ncbi.nlm.nih.gov/31474569/

Applications

Methods	Biomarkers	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

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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Verteporfin YAP inhibitor

Chemical Structure

Molecular Weight: 718.79