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.
For research use only. We do not sell to patients.
- CAS No.: 64118-86-1
- Formula: C9H14N4O
- Molecular Weight:194.23
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Storage:
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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. Further protocols information, click here.
In Vivo
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 No. 64118-86-1
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Molecular Weight 194.23
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Purity & Documentation
References
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Azimexon Related Classifications
HY-182506 Related Classifications
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