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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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Azimexon

Azimexon Chemical Structure

CAS No. : 64118-86-1

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Description

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[1][2][3].

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.

In Vivo

Azimexon (BM 12.531) (5-50 mg/kg; i.p.; single dose on day 0) produces 100% survival in CD2F1 mice receiving 500 R whole body irradiation at 50 mg/kg, while 20 mg/kg produces 100% survival in mice receiving 560 R irradiation[1].
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.

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]
Dosage: 5 mg/kg (500 R irradiation); 20 mg/kg (560 R/590 R irradiation); 50 mg/kg (500 R irradiation)
Administration: i.p.; single dose on day 0
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.
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]
Dosage: 2.5 mg/kg; 25 mg/kg; 250 mg/kg
Administration: i.p.; single dose on day 0
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.
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]
Dosage: 100 mg/kg
Administration: i.p.; two doses on days 9 and 16
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.
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]
Dosage: 50 mg/kg (single dose); 50 mg/kg (four doses); 50 mg/kg (six doses)
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
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.
Molecular Weight

194.23

Formula

C9H14N4O

CAS No.
SMILES

N#CC1N(C(C)(C)N2CC2C(N)=O)C1

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Azimexon
Cat. No.:
HY-182506
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