Verteporfin

別名:CL 318952

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。

Verteporfin化学構造

CAS No. 129497-78-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 50500 国内在庫なし(納期7~10日)
JPY 48000 国内在庫あり
JPY 145500 国内在庫あり
JPY 250500 国内在庫なし(納期7~10日)
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]
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文献中Selleckの製品使用例(131)

製品安全説明書

現在のバッチを見る: 純度: 99.31%
99.31

Verteporfin関連製品

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 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。
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
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

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

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

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)

mg/kg g μL

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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