Mitoxantrone (mitozantrone) |
| カタログ番号GC32714 |
Mitoxantrone (mitozantrone)は抗腫瘍誘導体である。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 65271-80-9
Sample solution is provided at 25 µL, 10mM.
Mitoxantrone (mitozantrone)は抗腫瘍誘導体である。MitoxantroneはトポイソメラーゼIIの強力な阻害剤としてDNAの複製を阻害し、水素結合の挿入を介してDNAへの単一および二鎖切断を誘発できる。Mitoxantroneはミトコンドリアのモノトランソルポーター（MCU）の阻害剤であり、ミトコンドリアに入るカルシウムを阻害し、ミトコンドリアのカルシウム過負荷を防ぐことができる[1-3]。
MitoxantroneはまたIC50が8.5 µmのプロテインキナーゼC（PKC）の活性を阻害する。Mitoxantrone（0.5µg/mL; 48H）はDNA断片化を誘発し、ポリ（ADP-リボース）ポリメラーゼ（PARP）のタンパク質の分解切断を誘発する。Mitoxantroneの細胞毒性効果がアポトーシスの誘発によるものである[4]。 Mitoxantrone（50 nm; 24 h）はLMH細胞（脂肪症細胞モデル）におけるトリグリセリド（TG）レベルと総コレステロール値を低下させる。Mitoxantroneはブロイラーの肝臓脂肪症を改善し、ブロイラーの循環脂質レベルと脂肪蓄積を減少させる[5]。
Mitoxantrone（0-3.2 mg/kg/day; i.p;腫瘍接種後の1、5と9日目）が処理した後、腫瘍を含んでいる鼠の寿命（IL）は100％以上増加する[6]。Mitoxantroneは体内のB細胞を阻害し続き、好中球と免疫調節CD8（低） Ｔ細胞の濃縮を引き起こす[7]。
References:
[1]. Nathanson L. Mitoxantrone. Cancer Treat Rev. 1984 Dec;11(4):289-93. doi: 10.1016/0305-7372(84)90025-2. PMID: 6534511.
[2]. Durr FE, Wallace RE, et,al. Molecular and biochemical pharmacology of mitoxantrone. Cancer Treat Rev. 1983 Dec;10 Suppl B:3-11. doi: 10.1016/0305-7372(83)90016-6. PMID: 6362876.
[3]. Arduino DM, Wettmarshausen J, et,al. Systematic Identification of MCU Modulators by Orthogonal Interspecies Chemical Screening. Mol Cell. 2017 Aug 17;67(4):711-723.e7. doi: 10.1016/j.molcel.2017.07.019. PMID: 28820965; PMCID: PMC5825229.
[4]. Bellosillo B, Colomer D, et,al. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6. doi: 10.1046/j.1365-2141.1998.00520.x. PMID: 9450803.
[5]. Vibet S, MahÉo K, et,al. Differential subcellular distribution of mitoxantrone in relation to chemosensitization in two human breast cancer cell lines. Drug Metab Dispos. 2007 May;35(5):822-8. doi: 10.1124/dmd.106.013474. Epub 2007 Feb 12. PMID: 17296624.
[6]. Fujimoto S, Ogawa M. Antitumor activity of mitoxantrone against murine experimental tumors: comparative analysis against various antitumor antibiotics. Cancer Chemother Pharmacol. 1982;8(2):157-62. doi: 10.1007/BF00255476. PMID: 7105379.
[7]. Chanvillard C, Millward JM, et,al. Mitoxantrone induces natural killer cell maturation in patients with secondary progressive multiple sclerosis. PLoS One. 2012;7(6):e39625. doi: 10.1371/journal.pone.0039625. Epub 2012 Jun 29. PMID: 22768101; PMCID: PMC3387260.
| 細胞実験[１]: | |
細胞株 | B-慢性リンパ球性白血病（B-CLL）細胞 |
準備方法 | 細胞が0.5 µg/mlのMitoxantroneと４８時間孵化する。 |
反応条件 | 0.5µg/ml; 48H |
アプリケーション | MitoxantroneはB-CLLリンパ球のアポトーシスを誘発する。 |
| 動物実験 [２]: | |
動物モデル | BDFメス鼠（L1210細胞腫瘍モデル） |
準備方法 | 一般に、腫瘍接種後の１、５と９日目にIPまたはIVの薬物を投与する。 |
投与形態 | 0-3.2 mg/kg/day; i.p;腫瘍接種後の１、５と９日目 |
アプリケーション | 静脈内投与した後、腫瘍が含んでいる鼠の寿命（IL）が100％以上増加する。 |
| References: [1]. Bellosillo B, Colomer D, et,al. Mitoxantrone, a topoisomerase II inhibitor, induces apoptosis of B-chronic lymphocytic leukaemia cells. Br J Haematol. 1998 Jan;100(1):142-6. doi: 10.1046/j.1365-2141.1998.00520.x. PMID: 9450803. | |
| Cas No. | 65271-80-9 | SDF | |
| Canonical SMILES | O=C1C2=C(C(NCCNCCO)=CC=C2NCCNCCO)C(C3=C(O)C=CC(O)=C13)=O | ||
| Formula | C22H28N4O6 | M.Wt | 444.48 |
| 溶解度 | DMSO : ≥ 150 mg/mL (337.47 mM) | Storage | -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2498 mL | 11.2491 mL | 22.4982 mL |
| 5 mM | 450 μL | 2.2498 mL | 4.4996 mL |
| 10 mM | 225 μL | 1.1249 mL | 2.2498 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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