Azimexon
Azimexon (BM 12.531) is an orally active immunomodulator with radioprotective and antitumor activities. Azimexon prolongs survival in multiple mouse models, enhances immunity and hematopoiesis, and alleviates radiation injury and tumor metastasis. Azimexon causes reversible hemolytic anemia in rats and dogs, and exerts therapeutic activity against adjuvant-induced arthritis in rats. Azimexon can be used for the research of lung carcinoma, leukemia, multiple myeloma, lung tumor, arthritis, breast cancer and AIDS‑related complex.
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- CAS. Nr.: 64118-86-1
- Formel: C9H14N4O
- Molecular Weight:194.23
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Azimexon (0.01-4.0 μg/mL; 12 h) slightly enhances NK cell cytotoxicity against K562, IGR3, and L1210 cells at concentrations of 0.01-0.25 μg/mL, inhibits NK activity at concentrations above 1 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Azimexon (2.5-250 mg/kg; i.p.; single dose on day 0) at 2.5 mg/kg significantly enhances the delayed-type hypersensitivity reaction in normal CD2F1 mice[1].
Azimexon (100 mg/kg; i.p.; two doses on days 9 and 16) significantly prolongs mean survival time by 31.8% in BALB/c mice bearing M109 alveolar carcinoma[1].
Azimexon (50 mg/kg; i.p.; six doses on days 8, 11, 13, 15, 18, 20) significantly augments Cytoxan therapy for L1210 leukemia in CD2F1 mice[1].
Azimexon acts synergistically with antibiotics to control lethal bacterial and fungal infections in mice[2].
Azimexon exhibits an antitumor effect in mouse tumor models[2].
Azimexon induces multiple immunomodulatory effects including leukocytosis, delayed-type hypersensitivity stimulation, and macrophage activation in Mus musculus and Rattus norvegicus[2].
Azimexon exhibits activity against adjuvant-induced arthritis in SD rats and stimulates bone marrow by increasing colony forming units[3].
Azimexon markedly reduces x-radiation toxicity in SD rats[3].
Azimexon (1-3 g/kg; p.o., i.p.; single dose) has low acute toxicity, with an oral LD50 of 1 g/kg in mice and 3 g/kg in rats, and an intraperitoneal LD50 of 1.5 g/kg in both species[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD2F1 (male, 6 to 10 weeks old, ~23 g, whole body X-ray irradiation at 500 R/560 R/590 R on day 0)[1]
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Dosage:5 mg/kg (500 R irradiation); 20 mg/kg (560 R/590 R irradiation); 50 mg/kg (500 R irradiation)
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Administration:i.p.; single dose on day 0
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Result:Achieved 90% survival and a mean survival time of 19.6 days at 5 mg/kg under 500 R irradiation.
Achieved 100% survival and a mean survival time of 20.0 days at 50 mg/kg under 500 R irradiation.
Achieved 100% survival and a mean survival time of 29.0 days at 20 mg/kg under 560 R irradiation without obvious body weight loss.
Showed no significant improvement in survival rate or mean survival time at 20 mg/kg under 590 R irradiation.
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Animal Model:CD2F1 (male, 6 to 10 weeks old, ~23 g, delayed-type hypersensitivity assay via s.c. injection of 1 × 108 sheep red blood cells on day 0 and day 4)[1]
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Dosage:2.5 mg/kg; 25 mg/kg; 250 mg/kg
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Administration:i.p.; single dose on day 0
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Result:Increased footpad swelling by 0.55 mm (229% of SRBC control) at 2.5 mg/kg.
Increased footpad swelling by 0.33 mm (138% of SRBC control) at 25 mg/kg.
Increased footpad swelling by 0.33 mm (138% of SRBC control) at 250 mg/kg.
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Animal Model:BALB/c (male, 6 to 10 weeks old, ~23 g, i.v. injection of 1 × 105 viable M109 alveolar carcinoma cells on day 0)[1]
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Dosage:100 mg/kg
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Administration:i.p.; two doses on days 9 and 16
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Result:Increased mean survival time from 13.2 days (untreated) to 17.4 days.
Resulted in 62% of treated mice surviving to day 16, compared to 0% of untreated mice.
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Animal Model:CD2F1 (male, 6 to 10 weeks old, ~23 g, s.c. injection of 1 × 104 viable L1210 leukemia cells on day 0)[1]
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Dosage:50 mg/kg (single dose); 50 mg/kg (four doses); 50 mg/kg (six doses)
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Administration:i.p.; single dose on day 8; four doses on days 8, 11, 13, 15; six doses on days 8, 11, 13, 15, 18, 20
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Result:Increased mean survival time and survival rate at day 45 in a dose‑dependent manner following Cytoxan treatment, reaching 40.5 days and 70% with six 50 mg/kg doses.
Chemical Information
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CAS. Nr. 64118-86-1
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Molecular Weight 194.23
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Formel C9H14N4O
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SMILES
N#CC1N(C(C)(C)N2CC2C(N)=O)C1
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Synonyms
BM 12.531
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Stylos WA, et al. The immunomodulatory effect on BM 12.531 (azimexon) on normal or tumored mice: in vitro and in vivo studies. J Immunopharmacol. 1980;2(1):113-132. [Content Brief]
[2]. Peter HH, et al. The effect of BM 12.531 (azimexon) on natural killer cell activity in myeloma patients. Eur J Cancer Clin Oncol. 1984;20(3):353-359. [Content Brief]
[3]. Remers WA, et al. Chemistry and pharmacology of imexon and related cyanoaziridines. Curr Med Chem. 2012;19(33):5745-53. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Azimexon Related Classifications
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