Mitonafide
(Synonyms: NSC 300288) 目录号 : GC67716Mitonafide (NSC 300288) 是一种细胞生长抑制剂。Mitonafide 通过嵌入 DNA 而与双链 DNA 结合,抑制 DNA 和 RNA 的合成。Mitonafide 是一种抗肿瘤剂,可用于癌症研究,如非小细胞肺癌 (NSCLC)、白血病。
Cas No.:54824-17-8
Sample solution is provided at 25 µL, 10mM.
Mitonafide (NSC 300288) is a cytostatic agent. Mitonafide binds to double-stranded DNA through intercalation, and inhibits DNA and RNA synthesis. Mitonafide is an antitumor agent that can be used in the research of cancers, such as non-small cell lung cancer (NSCLC), leukemia[1][2][3].
Mitonafide inhibits DNA and RNA synthesis and induces single-strand breaks in the DNA of chinese hamster ovary cells[1].
The incubation of Mitonafide with rat liver microsomes and NADPH under anaerobic conditions results in the formation of a metabolite identified as 5-aminomitonafide[2].
Mitonafide (25, 50 μM, 1 h) induces single-stand breaks in the DNA of L1210 cells[2].
Mitonafide (10-100 μM) exhibits cytotoxic effect in the HOP-62 lung cell line[4].
Cell Viability Assay[6]
Cell Line: | SK-OV-3, HepG2, A-549, T-24, SMMC-7721, HL-7702 |
Concentration: | 0-100 μM respectively. |
Incubation Time: | 48 h |
Result: | Inhibited cell viability with IC50 values of 6.26, 10.88, 7.94, 5.01, 6.94, 8.51 μM. |
Mitonafide (0.5 and 1 mg/kg, i.p., 1-7 days) shows antitumoral potency in S-180 bearing mice[4].
Mitonafide (5 mg/kg, i.p., twice a day) shows anticancer activity in HepG2 xenograft model[6].
Mitonafide (single i.p. injection, S-180 bearing mice) shows the LD50 value of 10.0 mg/kg[5].
Animal Model: | S-180 bearing mice[4] |
Dosage: | 0.5 mg/kg and 1 mg/kg |
Administration: | Intraperitoneal injection (i.p.) for 1-7 days |
Result: | Increased in median survival times. |
Animal Model: | HepG2 xenograft model [6] |
Dosage: | 5 mg/kg |
Administration: | Intraperitoneal injection (i.p.), twice a day. |
Result: | Exhibited a relative tumor increment rates (T/C) value of 28.8%. |
[1]. Llombart M, et al. Phase I study of mitonafide in solid tumors. Invest New Drugs. 1992 Aug;10(3):177-81.
[2]. inha BK, et al. Mechanism of DNA strand breaks by mitonafide, an imide derivative of 3-nitro-1,8-naphthalic acid. Biochem Pharmacol. 1985 Nov 1;34(21):3845-52.
[3]. Rosell R, et al. Phase I study of mitonafide in 120 hour continuous infusion in non-small cell lung cancer. Invest New Drugs. 1992 Aug;10(3):171-5.
[4]. Samanta S, et al. Antitumor activity of Nitronaphthal-NU, a novel mixed-function agent. J Exp Ther Oncol. 2005;5(1):15-22.
[5]. Pain A, et al. Evaluation of naphthalmustine, a nitrogen mustard derivative of naphthalimide as a rationally-designed anticancer agent. J Exp Clin Cancer Res. 2003 Sep;22(3):411-8.
[6]. Xin M, et al. Design, synthesis and biological evaluation of 3-nitro-1,8-naphthalimides as potential antitumor agents. Bioorg Med Chem Lett. 2020 Apr 15;30(8):127051.
Cas No. | 54824-17-8 | SDF | Download SDF |
别名 | NSC 300288 | ||
分子式 | C16H15N3O4 | 分子量 | 313.31 |
溶解度 | DMSO : 62.5 mg/mL (199.48 mM; Need ultrasonic) | 储存条件 | Store at -20°C |
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制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.1917 mL | 15.9586 mL | 31.9173 mL |
5 mM | 0.6383 mL | 3.1917 mL | 6.3835 mL |
10 mM | 0.3192 mL | 1.5959 mL | 3.1917 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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