Cat. No.: HY-106289

Antibiotic MX 2

Antibiotic MX 2 is an orally active antibiotic that can cross the blood-brain barrier. Antibiotic MX 2 inhibits the growth of drug-sensitive and multidrug-resistant tumor cells, prolongs the survival of tumor-bearing mice, induces single-strand and double-strand DNA breaks, suppresses colony formation of fresh human-derived tumor cells, and overcomes multidrug resistance mediated by P-glycoprotein. Antibiotic MX 2 can be used in research related to L1210 leukemia, Lewis lung cancer, colon adenocarcinoma type 26 and type 38, gastric adenocarcinoma, non-small cell lung cancer, mammary adenocarcinoma, drug-resistant P388 leukemia, renal cancer, melanoma, ovarian cancer, breast cancer, small cell lung cancer, and colorectal cancer.

For research use only. We do not sell to patients.

CAS No.: 105026-50-4
Formula: C₃₀H₃₅NO₁₁
Molecular Weight:585.61

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Please store the product under the recommended conditions in the Certificate of Analysis.

Antibiotic MX 2 Chemical Structure

CAS No.: 105026-50-4

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

All Antibiotic Isoforms :

In Vitro

Anti-cancer

Antibiotic MX 2 (Graded nM concentrations; 72 h) potently inhibits the growth of sensitive P388 leukemia cells with an IC₅₀ of 8.5 nM, and drug-resistant P388 sublines (P388/ADM, P388/ACR, P388/MMC) show minimal cross-resistance to the compound^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay^[1]

Cell Line:

P388, P388/ADM, P388/ACR, P388/MMC
Concentration:

Graded nM concentrations
Incubation Time:

72 h
Result:

Inhibited growth of sensitive P388 cells with an IC₅₀ of 8.5 nM.
Inhibited growth of P388/ADM cells with an IC₅₀ of 12.9 nM, showing 1.5-fold resistance relative to sensitive P388.
Inhibited growth of P388/ACR cells with an IC₅₀ of 12.7 nM, showing 1.5-fold resistance relative to sensitive P388.
Inhibited growth of P388/MMC cells with an IC₅₀ of 10.1 nM, showing 1.2-fold resistance relative to sensitive P388.

In Vivo

Anti-cancer

Antibiotic MX 2 (0.44-5 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 produces a maximum ILS of 270% and cures 3/6 mice at 3.33 mg/kg in female CD2F₁ mice bearing i.p.-inoculated L1210 leukemia^[1].
Antibiotic MX 2 (0.375-3 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 produces a maximum ILS of 240% at 1.5 mg/kg and cures 6/7 mice at 3 mg/kg in female CD2F₁ mice bearing i.v.-inoculated L1210 leukemia^[1].
Antibiotic MX 2 (0.375-3 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 achieves a maximum tumor growth inhibition with a T/C of 4% at 3 mg/kg in female BD2F₁ mice bearing s.c.-implanted Lewis lung carcinoma^[1].
Antibiotic MX 2 (1.33-3 mg/kg; i.v.; Days 1, 8, 15, 22) administered i.v. on Days 1, 8, 15, and 22 achieves a maximum tumor growth inhibition with a T/C of 15% and maximum ILS of 54% at 3 mg/kg, curing 2/10 mice in female CD2F₁ mice bearing s.c.-implanted colon adenocarcinoma 26^[1].
Antibiotic MX 2 (0.5-4 mg/kg; i.v.; Days 1, 8, 15, 22) administered i.v. on Days 1, 8, 15, and 22 achieves a maximum tumor growth inhibition with a T/C of 1% at 4 mg/kg and maximum ILS of 48% at 2, 3, and 4 mg/kg, with 5/6 survivors at 3 mg/kg in female BD2F₁ mice bearing s.c.-inoculated colon adenocarcinoma 38^[1].
Antibiotic MX 2 (2 mg/kg; i.v.; every 4 days; 3 total doses) administered at 2 mg/kg i.v. every 4 days for 3 total doses is effective (T/C ≤50% with statistical significance) against 3/4 gastric adenocarcinomas, 1/2 non-small-cell lung carcinomas, and 2/2 mammary adenocarcinomas, including a marked effect against MX-1 mammary adenocarcinoma, in female BALB/c-nu/nu athymic nude mice bearing human tumor xenografts^[1].
Antibiotic MX 2 (0.38-1.48 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 produces a maximum ILS of 87% at 1.48 mg/kg in female CD2F₁ mice bearing i.p.-inoculated ADM-resistant P388/ADM leukemia^[1].
Antibiotic MX 2 (0.48-2.5 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 produces a maximum ILS of 94% at 2.5 mg/kg in female CD2F₁ mice bearing i.p.-inoculated ACR-resistant P388/ACR leukemia^[1].
Antibiotic MX 2 (1.25-2.5 mg/kg; i.v.; Days 1, 5, 9) administered i.v. on Days 1, 5, and 9 produces a maximum ILS of 86% at 2.5 mg/kg in female CD2F₁ mice bearing i.p.-inoculated MMC-resistant P388/MMC leukemia^[1].
MX2 exhibits potent anti-leukemic activity in mice, doubling lifespan relative to doxorubicin in L1210-bearing mice and increasing lifespan by 90% in mice with multidrug-resistant P388 leukemia^[2].
MX2 demonstrates greater in vivo antitumor activity than doxorubicin against murine Lewis lung carcinoma and colon adenocarcinoma 26 and 38 models^[2].
MX2 significantly improves survival in rats with Walker 256 carcinosarcoma-induced meningeal carcinomatosis^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

CD2F₁ (female; i.p. inoculation of 10⁵ L1210 leukemia cells)^[1]
Dosage:

0.44 mg/kg; 0.66 mg/kg; 0.99 mg/kg; 1.48 mg/kg; 2.22 mg/kg; 3.33 mg/kg; 5 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced mean survival time (MST) of 9.7 days and increase in life-span (ILS) of 28% with 0/6 cured mice at 0.44 mg/kg.
Produced MST of 11.7 days and ILS of 55% with 0/6 cured mice at 0.66 mg/kg.
Produced MST of 14.5 days and ILS of 92% with 0/6 cured mice at 0.99 mg/kg.
Produced MST of 19.0 days and ILS of 151% with 0/6 cured mice at 1.48 mg/kg.
Produced MST of 23.2 days and ILS of 206% with 1/6 cured mice at 2.22 mg/kg.
Produced MST of 28.0 days and ILS of 270% with 3/6 cured mice at 3.33 mg/kg.
Produced MST of 11.3 days and ILS of 49% with 0/6 cured mice and observed toxicity at 5 mg/kg.

Animal Model:

CD2F₁ (female; i.v. inoculation of 10⁵ L1210 leukemia cells)^[1]
Dosage:

0.375 mg/kg; 0.75 mg/kg; 1.5 mg/kg; 3 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced mean survival time (MST) of 8.1 days and increase in life-span (ILS) of 37% with 0/7 cured mice at 0.375 mg/kg.
Produced MST of 13.6 days and ILS of 131% with 0/7 cured mice at 0.75 mg/kg.
Produced MST of 20.1 days and ILS of 240% with 0/7 cured mice at 1.5 mg/kg.
Produced MST of 12.0 days and ILS of 102% with 6/7 cured mice at 3 mg/kg.

Animal Model:

BD2F₁ (female; s.c. implantation of 2×2×2 mm Lewis lung carcinoma fragments)^[1]
Dosage:

0.375 mg/kg; 0.75 mg/kg; 1.5 mg/kg; 3 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced tumor volume of 1570 mm³ and T/C of 107% with 0/10 cured mice at 0.375 mg/kg.
Produced tumor volume of 1260 mm³ and T/C of 86% with 0/10 cured mice at 0.75 mg/kg.
Produced tumor volume of 372 mm³ and T/C of 25% with 1/10 cured mice at 1.5 mg/kg.
Produced tumor volume of 57 mm³ and T/C of 4% with 1/10 cured mice at 3 mg/kg.

Animal Model:

CD2F₁ (female; s.c. implantation of 2×2×2 mm colon adenocarcinoma 26 fragments)^[1]
Dosage:

1.33 mg/kg; 2 mg/kg; 3 mg/kg
Administration:

i.v.; Days 1, 8, 15, 22
Result:

Produced tumor volume of 487 mm³, T/C of 63%, median survival time (MST) of 36.5 days, increase in life-span (ILS) of 6% with 0/10 cured mice at 1.33 mg/kg.
Produced tumor volume of 309 mm³, T/C of 40%, MST of 42.3 days, ILS of 23% with 0/10 cured mice at 2 mg/kg.
Produced tumor volume of 115 mm³, T/C of 15%, MST of 53.0 days, ILS of 54% with 2/10 cured mice at 3 mg/kg.

Animal Model:

BD2F₁ (female; s.c. inoculation of colon adenocarcinoma 38 tumor brei)^[1]
Dosage:

0.5 mg/kg; 1 mg/kg; 2 mg/kg; 3 mg/kg; 4 mg/kg
Administration:

i.v.; Days 1, 8, 15, 22
Result:

Produced tumor volume of 737 mm³, T/C of 102%, median survival time (MST) of 57.0 days, increase in life-span (ILS) of 39% with 2/6 survivors on Day 61 at 0.5 mg/kg.
Produced tumor volume of 267 mm³, T/C of 37%, MST of 55.0 days, ILS of 34% with 1/6 survivors on Day 61 at 1 mg/kg.
Produced tumor volume of 96 mm³, T/C of 13%, MST of 60.9 days, ILS of 48% with 4/6 survivors on Day 61 at 2 mg/kg.
Produced tumor volume of 39 mm³, T/C of 5%, MST of 61.0 days, ILS of 48% with 5/6 survivors on Day 61 at 3 mg/kg.
Produced tumor volume of 7 mm³, T/C of 1%, MST of 60.7 days, ILS of 48% with 3/6 survivors on Day 61 and observed toxicity at 4 mg/kg.

Animal Model:

BALB/c-nu/nu athymic nude (female; s.c. implantation of human tumor fragments; treatment initiated when tumors reached 100-300 mm³)^[1]
Dosage:

2 mg/kg
Administration:

i.v.; every 4 days; 3 total doses
Result:

Achieved T/C of 37% (statistically significant) against gastric adenocarcinoma Sc-2.
Achieved T/C of 43% against gastric adenocarcinoma Sc-6.
Achieved T/C of 36% (statistically significant) against gastric adenocarcinoma Sc-9.
Achieved T/C of 43% (statistically significant) against gastric adenocarcinoma St-4.
Achieved T/C of 85% against small-cell lung carcinoma LX-1.
Achieved T/C of 57% against non-small-cell lung carcinoma Lu-24.
Achieved T/C of 37% (statistically significant) against non-small-cell lung carcinoma Lu-99.
Achieved T/C of 0.2% (statistically significant) against mammary adenocarcinoma MX-1.
Achieved T/C of 32% (statistically significant) against mammary adenocarcinoma H-31.

Animal Model:

CD2F₁ (female; i.p. inoculation of 10⁶ P388/ADM leukemia cells)^[1]
Dosage:

0.38 mg/kg; 1.48 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced increase in life-span (ILS) of 30% at 0.38 mg/kg.
Produced maximum ILS of 87% at 1.48 mg/kg.

Animal Model:

CD2F₁ (female; i.p. inoculation of P388/ACR leukemia cells)^[1]
Dosage:

0.48 mg/kg; 2.5 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced increase in life-span (ILS) of 30% at 0.48 mg/kg.
Produced maximum ILS of 94% at 2.5 mg/kg.

Animal Model:

CD2F₁ (female; i.p. inoculation of P388/MMC leukemia cells)^[1]
Dosage:

1.25 mg/kg; 2.5 mg/kg
Administration:

i.v.; Days 1, 5, 9
Result:

Produced increase in life-span (ILS) of 81% at 1.25 mg/kg.
Produced maximum ILS of 86% at 2.5 mg/kg.

Related Protocols :

Chemical Information

CAS No. 105026-50-4
Molecular Weight 585.61
Formula C₃₀H₃₅NO₁₁
SMILES

O=C1C=2C=CC=C(O)C2C(=O)C=3C(O)=C4C(=C(O)C13)C(O)C(O)(CC)CC4OC5OC(C)C(O)C(N6CCOCC6)C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Watanabe M, et al. MX2, a morpholino anthracycline, as a new antitumor agent against drug-sensitive and multidrug-resistant human and murine tumor cells. Cancer Res. 1988 Dec 1;48(23):6653-7. [Content Brief]

[2]. Ebrahim el-Zayat AA, et al. Activity of the morpholino anthracycline 3'-deamino-3'-morpholino-13-deoxo-10-hydroxycarminomycin (MX2) against human tumor colony-forming units in vitro. Investigational new drugs. 1995;13(2):125-131. [Content Brief]

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Antibiotic MX 2

All Antibiotic Isoforms