1. Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Topoisomerase
    ADC Cytotoxin

DOXO-EMCH (Synonyms: Doxorubicin-EMCH)

Cat. No.: HY-16261A
Handling Instructions

DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.

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

DOXO-EMCH Chemical Structure

DOXO-EMCH Chemical Structure

CAS No. : 151038-96-9

Size Price Stock
5 mg USD 162 Get quote
10 mg USD 209 Get quote
50 mg USD 714 Get quote
100 mg USD 1048 Get quote

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Other In-stock Forms of DOXO-EMCH:

Other Forms of DOXO-EMCH:

    DOXO-EMCH purchased from MCE. Usage Cited in: Br J Pharmacol. 2017 Sep;174(17):2862-2879.

    HSA decorated with Cy7 could be imaged. Through this strategy, the drug distribution of the HSA-decorated form and unbound form are imaged, and the merge rates are also calculated.

    DOXO-EMCH purchased from MCE. Usage Cited in: ACS Med Chem Lett. 2015 Jun 22;6(8):948-52.

    Combination treatment. (a) Comparison of AZD-8055 and ABT-263 treatment in all cell lines. Red indicates sensitivity, while blue indicates resistance. (b) Depiction of synergism where the values shown are excess over Bliss Independence, a prediction of inhibition without synergism. Increased synergism is evident by an increased number, shown in red, while negative numbers in blue represent an antagonistic effect.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin, is an albumin binding prodrug.

    IC50 & Target[1]

    Topoisomerase II

     

    In Vitro

    DOXO-EMCH is an an acid-sensitive prodrug of Doxorubicin that binds rapidly and selectively to the cysteine-34 position of circulating albumin[1].

    In Vivo

    DOXO-EMCH is a 6-maleimidocaproyl hydrazone derivative of Doxorubicin. DOXO-EMCH unlike its free Doxorubicin parent, achieves complete remissions in a murine renal cell carcinoma model and in 2 breast carcinoma xenograft models. Moreover, DOXO-EMCH is also superior to Doxorubicin with regard to drug toxicity in mice, rats and dogs, and exhibits a good safety profile[2].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.3320 mL 6.6600 mL 13.3200 mL
    5 mM 0.2664 mL 1.3320 mL 2.6640 mL
    10 mM 0.1332 mL 0.6660 mL 1.3320 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      DOXO-EMCH is prrpared in PBS[3].

    References
    Animal Administration
    [2]

    Rats[2]
    Male Wistar rats are housed in a normal night–day rhythm under standard conditions of temperature, humidity and fed a normal rat chow. At 10 weeks of age, the rats receive an intravenous port under anesthesia. Based on the mortality in earlier investigations, the rats are divided into 4 experimental groups of different size: 9 animals served as controls (Group A) and received intravenous saline (300-700 μL). Group B (n=15) receive equivalent volumes of Doxorubicin at a dose of 0.8 mg/kg, freshly dissolved in water from lyophilized powder. Group C, the DOXO-EMCH low-dose group (n=10), receive intravenous DOXO-EMCH, freshly reconstituted in sterile 10 mM sodium phosphate, 5 %D-(+)-glucose (pH 6.4) and at a dose equivalent to 0.8 mg/kg of free Doxorubicin (1.1 mg/kg). Group D (n=10) is injected with a higher dose of DOXO-EMCH (3.3 mg/kg), a dose that with respect to subacute mortality is equitoxic to 0.8 mg/kg of Doxorubicin in a 4-cycle repeat dose study in rats. All animals receive 7-weekly injections through the port, beginning at 11 weeks of age and are killed by cervical dislocation at 48 weeks of age, immediately before postmortem examination and organ collection. Heart weights are recorded. Left ventricle and apex are snap frozen and cryopreserved in liquid nitrogen until subsequent analysis. Aliquots are fixed in glutaraldehyde (3%) for subsequent electron microscopy.

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

    References
    Molecular Weight

    750.75

    Formula

    C₃₇H₄₂N₄O₁₃

    CAS No.

    151038-96-9

    SMILES

    [H][[email protected]@]1(O[[email protected]]2C[[email protected]@](/C(CO)=N\NC(CCCCCN3C(C=CC3=O)=O)=O)(O)CC(C2=C4O)=C(O)C5=C4C(C6=C(OC)C=CC=C6C5=O)=O)O[[email protected]@H](C)[[email protected]@H](O)[[email protected]@H](N)C1

    Storage

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

    Shipping

    Room temperature in continental US; may vary elsewhere

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