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Mitonafide

(Synonyms: NSC 300288) 目录号 : GC67716

Mitonafide (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。

Mitonafide Chemical Structure

Cas No.:54824-17-8

规格 价格 库存 购买数量
10mg
¥1,170.00
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25mg
¥2,250.00
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50mg
¥3,600.00
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100mg
¥5,850.00
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Sample solution is provided at 25 µL, 10mM.

Description

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.

化学性质

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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溶解性数据

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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
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