Home Angiogenesis VDA chemical Verteporfin

연구용

Verteporfin YAP inhibitor

제품 번호: S1786

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.
Verteporfin VDA chemical Chemical Structure

화학 구조

분자량: 718.79

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품질 관리 (Quality Control)

배치: 순도: 99.31%
99.31

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 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
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 718.79 화학식

C41H42N4O8

 보관 (수령일로부터) 3 years-20°C （in the dark）powder
CAS 번호 129497-78-5 SDF 다운로드 원액 보관

동의어 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

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (139.12 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
VDA
(Endothelial cells)
YAP/TEAD interaction
시험관 내(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.

생체 내(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.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/29438698/
  • [5] https://pubmed.ncbi.nlm.nih.gov/31474569/

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot ECAD / Vimentin / Sox2 / CD44 / CD133 c-Myc / Bcl-2 p-S6(S240/244) / p-4EBP1(S65) beta-catenin
S1786-WB4
30467925
Growth inhibition assay Cell viability
S1786-viability1
28042502
Immunofluorescence p-YAP(Y357) Calreticulin YAP1
S1786-IF3
28404908

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
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