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Verteporfin

別名: CL 318952 中文名稱：維替泊芬

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Verteporfin是一種能夠抑制YAP-TEAD相互作用的小分子化合物，抑制YAP誘導(dǎo)的肝臟過度生長。同時(shí)，它還是一種有效的衍生自卟啉的第二代光敏劑。Verteporfin 是一種自噬抑制劑。Verteporfin 可抑制細(xì)胞增殖并誘導(dǎo)凋亡。

Verteporfin Chemical Structure

Verteporfin Chemical Structure

CAS: 129497-78-5

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 2760.03 現(xiàn)貨
10mg 2607.44 現(xiàn)貨
50mg 7928.11 現(xiàn)貨
100mg 13677.3 現(xiàn)貨
1g 81818.1 現(xiàn)貨
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Verteporfin相關(guān)產(chǎn)品

相關(guān)信號通路圖

VDA Signaling Pathways

VDA信號通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
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

產(chǎn)品描述 Verteporfin是一種能夠抑制YAP-TEAD相互作用的小分子化合物，抑制YAP誘導(dǎo)的肝臟過度生長。同時(shí)，它還是一種有效的衍生自卟啉的第二代光敏劑。Verteporfin 是一種自噬抑制劑。Verteporfin 可抑制細(xì)胞增殖并誘導(dǎo)凋亡。
靶點(diǎn)
VDA [1]
(Endothelial cells)		 YAP/TEAD interaction [3]
體外研究(In Vitro)
體外研究活性

對于穿透組織最好的波長(i.e.，大約700 nm)下的吸收光，Verteporfin比hematoporphyrin大約有效4倍，從而比hematoporphyrin提供了更高的細(xì)胞毒性(在人貼壁細(xì)胞中10倍以上)。Verteporfin是親脂性的，與正常細(xì)胞或靜息細(xì)胞相比，更容易被惡性的或激活的細(xì)胞攝取。Verteporfin與LDL結(jié)合形成一個復(fù)合物，隨后可能通過LDL受體或者內(nèi)吞作用被增殖細(xì)胞 (例如，新生血管內(nèi)皮細(xì)胞) 攝取。Verteporfin療法通過血管通道中形成血栓實(shí)現(xiàn)新生血管區(qū)的血管造影完全閉塞，進(jìn)而引起選擇性血管內(nèi)皮損傷。Verteporfin療法選擇性誘導(dǎo)可再生的和離體的脈絡(luò)膜毛細(xì)血管閉塞，而不改變覆蓋的光感受器或神經(jīng)節(jié)細(xì)胞，如光學(xué)和電子顯微鏡所示。[1]

HL-60細(xì)胞中胱天蛋白酶-3和胱天蛋白酶-9的活化以及PARP的裂解映射出，光存在下，Verteporfin快速使細(xì)胞凋亡改變，該改變會被普通半胱天冬酶抑制劑ZVAD.fmk阻斷。[2]
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 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
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Verteporfin可用于脈絡(luò)膜血管和CNV的血管可視化，這表明光敏劑在猴子的實(shí)驗(yàn)性CNV中快速集聚。Verteporfin在建立的兔子眼睛的脈絡(luò)膜脈管系統(tǒng)，RPE，以及光感受器中迅速積累。在小鼠體內(nèi)，靜脈注射3小時(shí)后，Verteporfin達(dá)到最大組織水平，隨后在24小時(shí)內(nèi)迅速下降。Verteporfin在體內(nèi)代謝為活性較低的形式，并且迅速清除，主要通過糞便排泄，一小部分通過尿液排泄。Verteporfin療法有效的選擇性阻止了熒光染料從實(shí)驗(yàn)性誘導(dǎo)的猴子CNV的泄漏。[1]
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

化學(xué)信息&溶解度

分子量 718.79 分子式

C41H42N4O8
CAS號 129497-78-5 SDF Download Verteporfin SDF
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
儲存條件(自收到貨起) 3年 -20°C(避光) 粉狀

體外溶解度
批次：

DMSO : 100 mg/mL ( (139.12 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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