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.

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CAS No.: 105026-50-4
Formule: C₃₀H₃₅NO₁₁
Masse moléculaire:585.61

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Antibiotic MX 2 Chemical Structure

CAS No.: 105026-50-4

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
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Activité biologique

Description

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In Vitro

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

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.

Chemical Information

CAS No. 105026-50-4
Masse moléculaire 585.61
Formule 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
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[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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Antibiotic MX 2

Voir tous les produits spécifiques à Isoform Antibiotic

Activité biologique

Chemical Information

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Calculators

Help & FAQs

Antibiotic MX 2 Related Classifications

HY-106289 Related Classifications