Fosbretabulin (Combretastatin A4 Phosphate) Disodium

別名：CA 4DP

製品コード：S7204 純度：99.86%

Fosbretabulin (Combretastatin A4 Phosphate) Disodium is the water-soluble prodrug of Combretastatin A4 (CA4), which is a microtubule-targeting agent that binds β-tubulin with K_d of 0.4 μM in a cell-free assay. Fosbretabulin Disodium inhibits the polymerization of tubulin with IC50 of 2.4 μM, and also disrupts tumor vasculature. Fosbretabulin disodium induces mitotic arrest and apoptosis in endothelial cells. Phase 3.

Fosbretabulin (Combretastatin A4 Phosphate) Disodium化学構造

CAS No. 168555-66-6

サイズ	価格(税別)	在庫状況
10mg	JPY 26400	国内在庫あり
25mg	JPY 46800	国内在庫あり

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（11）

カスタマーフィードバック3个实验数据

製品安全説明書

Fosbretabulin (Combretastatin A4 Phosphate) Disodium関連製品

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シグナル伝達経路

Microtubule Associatedシグナル伝達経路

Microtubule Associated阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報	PMID
SKOV3 cells	Proliferation assay	Antiproliferative activity against human SKOV3 cells by sulforhodamine B assay, IC50=0.0045 μM	20973488
HeLa cells	Proliferation assay	Antiproliferative activity against human HeLa cells by sulforhodamine B assay, IC50=0.0047 μM	20973488
rat A10 cells	Function assay	Inhibition of microtubule depolymerization in rat A10 cells assessed as reorganization of interphase microtubule network by indirect immunofluorescence technique, EC50=0.007 μM	20973488
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生物活性

製品説明

特性

A microtubule associated inhibitor with higher affinity to β-tubulin vs. Colchicine. Best for advanced solid tumors, anaplastic thyroid cancer, & choroidal neovascularization.

Targets

Tubulin ^[1]
(Cell-free assay)

2.4 μM

In Vitro
In vitro	Fosbretabulin disodium (Combretastatin A-4 phosphate disodium, CA4P disodium) is the water-soluble prodrug of combretastatin A4 (CA4), which is originally isolated from African tree Combretum caffrum. CA4 is a tubulin-binding agent that binds at or near the colchicine binding site of β-tubulin (Kd = 0.40 μM), inhibits tubulin assembly with IC50 of 2.4 μM. ^[1] CA4 is cytotoxic towards proliferating but not quiescent endothelial cells, has potent and selective toxicity towards tumor vasculature. ^[2] CA4P (1 mM, 30 minutes) disrupts the endothelial microtubule cytoskeleton and mediates changes in endothelial cell morphology. CA4P stimulates actin stress fiber formation and membrane blebbing and increases monolayer permeability via Rho/Rho-kinase. ^[3] CA4P increases endothelial cell permeability, while inhibiting endothelial cell migration and capillary tube formation predominantly through disruption of VE-cadherin/β-catenin/Akt signaling pathway, thereby leading to rapid vascular collapse and tumor necrosis. ^[4]
Kinase Assay	Tubulin assembly-disassembly
Kinase Assay	The assembly of microtubules from isolated tubulin is carried out spectrophotometrically at 350 nm and utilises the increase in turbidity which is associated with microtubule formation. Assembly is initiated by temperature increase from 10 to 35 °C. The effect of drugs on the increase in light absorption is carried. Drugs are dissolved in DMSO (<4%), which does not affect control assembly
細胞実験	細胞株	HUVECs
	濃度	~50 nM
	反応時間	12-48 h
	実験の流れ	For the proliferation assay, the minimal concentration of FBS (1%) diluted in X-VIVO medium is used to allow sufficient viability of endothelial cells. After detachment, the cells are seeded at a concentration of 2×10⁴ HUVECs in each well of 24-well plates, allowed to adhere overnight, and then incubated with or without cytokines (5 ng/ml FGF-2 or 5 ng/ml VEGF-A). CA4P is added at 0 – 50 nM. After incubation for 12, 24, 36, and 48 hours, cells are detached by trypsin/EDTA and manually counted using trypan blue exclusion.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Immunofluorescence	tubulin / VE-cadherin Actin / N-cadherin / CD31		29221156

In Vivo
In Vivo	CA4P causes rapid, extensive and irreversible vascular shutdown in experimental tumor models following the administration of a single dose at 10% of the maximum tolerated dose (MTD). CA4P causes a 93% reduction in vascular volume 6 h following drug administration. ^[2] CA4P(100 mg/kg, 6 h following administration) reduces tumor blood by approximately 100-fold, compared with approximately 7-fold in the spleen. ^[5]
動物実験	動物モデル	BD9 rats implanted with tumor
	投与量	100 mg/kg, 3 ml/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 2024-01-11)
NCT02641639	Terminated	Platinum Resistant Ovarian Cancer	Mateon Therapeutics	June 2016	Phase 2\|Phase 3
NCT02055690	Terminated	Ovarian Neoplasms\|Neoplasms Ovarian\|Ovarian Cancer	The Christie NHS Foundation Trust\|Novartis\|Mateon Therapeutics\|East and North Hertfordshire NHS Trust	September 2014	Phase 1\|Phase 2
NCT01023295	Completed	Polypoidal Choroidal Vasculopathy	Mateon Therapeutics	July 2009	Phase 2

参考
[1] Woods JA, et al. Br J Cancer 1995, 71(4), 705-711. [2] Dark GG, et al. Cancer Res 1997, 57(10), 1829-1834. [3] Kathou C, et al. Blood, 2002, 99(6), 2060-2069. [4] Vincent L, et al. J Clin Invest, 2005, 115(11), 2992-3006. [5] Tozer GM, et al. Cancer Res, 1999, 59(7), 1626-1634. + 展開

参考

+ 展開

化学情報

分子量	440.29	化学式	C₁₈H₁₉O₈P.2Na
CAS No.	168555-66-6	SDF	Download Fosbretabulin (Combretastatin A4 Phosphate) Disodium SDFをダウンロードする
Smiles	COC1=C(C=C(C=C1)C=CC2=CC(=C(C(=C2)OC)OC)OC)OP(=O)([O-])[O-].[Na+].[Na+]
保管	3年-20°C粉	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年-20°C粉	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:

Water : 28 mg/mL

DMSO : Insoluble ( 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。)

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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Handling Instructions

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