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Amonafide

別名：NSC308847,AS1413

Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.

Amonafide化学構造

CAS No. 69408-81-7

サイズ 価格(税別) 在庫状況
JPY 34000 国内在庫あり
JPY 85500 国内在庫あり

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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文献中Selleckの製品使用例（8）

製品安全説明書

現在のバッチを見る： S136701 DMSO] 57 mg/mL] false] Ethanol] 4 mg/mL] false] Water] Insoluble] false 純度： 99.94%
99.94

Amonafide関連製品

シグナル伝達経路

Topoisomerase Signaling Pathways

Topoisomeraseシグナル伝達経路

Topoisomerase阻害剤の選択性比較

生物活性

製品説明 Amonafide (NSC308847, AS1413) produces protein-associated DNA-strand breaks through a topoisomerase II-mediated reaction, but does not produce topoisomerase I-mediated DNA cleavage. Phase 3.
Targets
Topo II [1]
In Vitro
In vitro Through a topoisomerase II-mediated reaction, Amonafide treatment produces DNA single-strand breaks (SSB), double-strand breaks (DSB), and DNA-protein cross-links in human myeloid leukemia cells. This compound treatment inhibits colony formation of the leukemic cell lines and the normal human bone marrow GM-CFC in a dose-dependent manner. It does not produce topoisomerase I-mediated DNA cleavage even at 100 μM. The m-AMSA-resistant line is less than 2-fold resistant to this compound [1] This chemical interferes with the DNA breakage-reunion activity of mammalian DNA topoisomerase II resulting in DNA cleavage stimulation. [2] Compared with those of other antitumor drugs, this compound-stimulated cleavage intensity patterns are markedly different. It highly prefers a cytosine, and excludes guanines and thymines instead, at position -1, with lower preference for an adenine at position +1. [3] Topoisomerase II-mediated DNA cleavage induced by this agent is affected only slightly (less than 3-fold) by 1 mM ATP, suggesting that it is an ATP-insensitive topoisomerase II inhibitor in contrast to doxorubicin, etoposide, and mitoxantrone. [4] This compound significantly inhibits the growth of HT-29, HeLa, and PC3 cells with IC50 of 4.67 μM, 2.73 μM, and 6.38 μM, respectively. [5] It is unaffected by P-glycoprotein-mediated efflux, unlike those of the classical topoisomerase II inhibitors (daunorubicin, doxorubicin, idarubicin, etoposide, and mitoxantrone). [6]
細胞実験 細胞株 HT-29, HeLa, and PC3
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 72 hours
実験の流れ All cell lines are in the logarithmic phase of growth when the assay of 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) is carried out. Cells are harvested and seeded into 96-well tissue culture plates at a density of 2.5 × 103 cells/well in 150 μL aliquots of medium. The concentrations tested are serial dilutions of a stock solution (10 μM in DMSO) with phosphate-buffered saline (PBS) and are added 24 hours later. The assay is ended after 72 hours of this compound exposure and PBS is used as a negative control. After 72 hours treatment, cells are washed twice with PBS, and then 50 μL/well of MTT reagent (1 mg/mL in PBS) together with 150 μL/well of prewarmed medium are added. The plates are returned to the incubator for 4 hours. Subsequently, DMSO is added as solvent. Absorbance is determined at 570 nm with a Microplate reader. All experiments are performed at least three times, and the average of the percentage absorbance is plotted against concentration. Then, the concentration of this chemical required to inhibit 50% of cell growth (IC50) is calculated for it.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01066494 Unknown status
Acute Myeloid Leukemia
Antisoma Research
 January 2010 Phase 2
NCT00273884 Completed
Acute Myeloid Leukemia
Xanthus Pharmaceuticals Inc.
 August 2005 Phase 2
NCT00087854 Completed
Prostate Cancer
Xanthus Pharmaceuticals Inc.
 March 2004 Phase 1|Phase 2
  • https://pubmed.ncbi.nlm.nih.gov/3026621/
  • https://pubmed.ncbi.nlm.nih.gov/2550774/
  • https://pubmed.ncbi.nlm.nih.gov/7862525/
  • https://pubmed.ncbi.nlm.nih.gov/11278845/
  • https://pubmed.ncbi.nlm.nih.gov/14998328/
  • https://pubmed.ncbi.nlm.nih.gov/17826829/

化学情報

分子量 283.33 化学式

C16H17N3O2
CAS No. 69408-81-7 SDF Download Amonafide SDFをダウンロードする
Smiles CN(C)CCN1C(=O)C2=CC=CC3=CC(=CC(=C32)C1=O)N
保管

In vitro
Batch:

DMSO : 57 mg/mL ( (201.17 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。)

Ethanol : 4 mg/mL

Water : 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 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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