1. Cytoskeleton
    Cell Cycle/DNA Damage
    Antibody-drug Conjugate/ADC Related
  2. Microtubule/Tubulin
    ADC Cytotoxin
  3. D8-MMAF

D8-MMAF (Synonyms: Monomethylauristatin F D8)

Cat. No.: HY-15579S
Handling Instructions

D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride. MMAF Hydrochloride, a potent tubulin polymerization inhibitor, is used as a antitumor agent and a cytotoxic component of antibody-drug conjugates (ADCs).

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

D8-MMAF Chemical Structure

D8-MMAF Chemical Structure

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Description

D8-MMAF hydrochloride is a deuterated form of MMAF hydrochloride. MMAF Hydrochloride, a potent tubulin polymerization inhibitor, is used as a antitumor agent and a cytotoxic component of antibody-drug conjugates (ADCs)[1].

IC50 & Target

Auristatin

 

In Vitro

MMAF shows in vitro cytotoxicity against a panel of cell lines. The IC50 values for Karpas 299, H3396, 786-O and Caki-1 are 119, 105, 257, and 200 nM, respectively. Targeted MMAF is much more potent than the free drug, and that cAC10 conjugates of MMAF display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF and is active on all the CD30-positive cell lines tested[1].

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

In Vivo

The maximum tolerated dose in mice of MMAF (>16 mg/kg) is much higher than MMAE (1 mg/kg). cAC10-L1-MMAF4 has an MTD of 50 mg/kg in mice and 15 mg/kg in rats. The corresponding cAC10-L4-MMAF4 ADC was much less toxic, having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats, respectively[1].

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

Molecular Weight

740.01

Formula

C₃₉H₅₇D₈N₅O₈

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
Cell Assay
[1]

Cells are treated with serial dilutions of test molecules and incubated 4-6 days depending on cell line. Assessment of cellular growth and data reduction to generate IC50 values is done using Alamar Blue dye reduction assay[2].

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

Animal Administration
[1]

Mice: When subcutaneous Karpas 299 tumor size reaches 300 mm3, three animals per group receives one injection of 10 mg antibody component/kg body weight of either cAC10-L1-MMAF4 or cBR96-L1-MMAF4 intravenously. Tumors are then removed and placed in optimal cutting temperature compound, and 5 μm-thin frozen tissue sections are stained using immunohistochemistry evaluation[1].

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

References
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D8-MMAF
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HY-15579S
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