[CAS NO. 54824-17-8] Mitonafide
PRODUCTS SPECIFICATIONS [54824-17-8]
DESCRIPTION [54824-17-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 313.31 |
| Molecular Formula | C16H15N3O4 |
| SMILES | O=C1N(C(C2=CC([N+]([O-])=O)=CC3=CC=CC1=C23)=O)CCN(C)C |
Summary
IC50 & Target
DNA and RNA synthesis [1]
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 IC 50 values of 6.26, 10.88, 7.94, 5.01, 6.94, 8.51 μM. |
In Vivo
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 LD
50
value of 10.0 mg/kg
[5]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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%. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 62.5 mg/mL ( 199.48 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 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 |
References
- [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.
Synonyms