Verteporfin

別名：CL 318952

製品コード：S1786 純度：99.59%

ベルテポルフィン (Verteporfin (CL 318952)) は、TEAD-YAP 相互作用 と YAP による肝肥大を阻害します。また、ポルフィリンに由来する強力な第 2 世代の光増感剤でもあります。ベルテポルフィンはオートファジー (autophagy) 阻害剤です。ベルテポルフィンは細胞増殖を阻害し、アポトーシス (apoptosis) を誘導します。

CAS No. 129497-78-5

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 50500	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり
100mg	JPY 250500	国内在庫あり
1g	JPY 745500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（139）

製品安全説明書

現在のバッチを見る：純度： 99.59%

99.59

Verteporfin関連製品

関連製品	Vadimezan (DMXAA) Plinabulin	もっと見る
関連化合物ライブラリー	Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Angiogenesis Related compound Library HIF-1 Signaling Pathway Compound Library FDA-approved Anticancer Drug Library	もっと見る

シグナル伝達経路

VDAシグナル伝達経路

VDA阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

Targets

VDA ^[1]
(Endothelial cells)

YAP/TEAD interaction ^[3]

In Vitro
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]
細胞実験	細胞株	Ki67+ and Sox10+ cells
	濃度	2 uM
	反応時間	72 h
	実験の流れ	Cells were treated with verteporfin (2 µM) for 72 hr for Brdu staining.
実験結果図	Methods	Biomarkers	結果図	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

In Vivo
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]
動物実験	動物モデル	Atoh1-Ptch mice
	投与量	100 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考
[1] Schmidt-Erfurth U, et al. Surv Ophthalmol, 2000, 45(3), 195-214. [2] Granville DJ, et al. Blood, 2000, 95(1), 256-262. [3] Liu-Chittenden Y, et al. Genes Dev. 2012, 26(12):1300-5. [4] Wu LMN, et al. Cancer Cell. 2018 Feb 12;33(2):292-308.e7. [5] Zhang L, et al. Cancer Cell. 2019 Sep 16;36(3):302-318.e7. + 展開

参考

+ 展開

化学情報

分子量	718.79	化学式	C₄₁H₄₂N₄O₈
CAS No.	129497-78-5	SDF	Download Verteporfin SDFをダウンロードする
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
保管	3 years-20°C （in the dark）powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3 years-20°C （in the dark）powder	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (139.12 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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