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

MMAF (Synonyms: Monomethylauristatin F)

Cat. No.: HY-15579
Handling Instructions

MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

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

MMAF Chemical Structure

MMAF Chemical Structure

CAS No. : 745017-94-1

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Description

MMAF (Monomethylauristatin F) is an antitubulin agent that inhibit cell division; attenuates its cytotoxic activity compared to MMAE. MMAF is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) to treat several different cancer types.

IC50 & Target

IC50: 119 nM (Cytotoxicity, Karpas 299 cell), 105 nM (Cytotoxicity, H3396 cell), 257 nM (Cytotoxicity, 786-O cell), 200 nM (Cytotoxicity, Caki-1, cell)[1]

In Vitro

MMAF (Monomethylauristatin F) 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 (Monomethylauristatin F) is much more potent than the free drug, and that cAC10 conjugates of MMAF (Monomethylauristatin F) display pronounced activities. On a molar basis, the cAC10-L1-MMAF4 is an average of over 2200-fold more potent than free MMAF (Monomethylauristatin F) and is active on all the CD30-positive cell lines tested[1].

In Vivo

The maximum tolerated dose in mice of MMAF (Monomethylauristatin F) (>16 mg/kg) is much higher than MMAF (Monomethylauristatin F) (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].

Molecular Weight

731.96

Formula

C₃₉H₆₅N₅O₈

CAS No.

745017-94-1

SMILES

CC(C)[[email protected]](NC)C(N[[email protected]](C(N([[email protected]@H]([[email protected]@H](C)CC)[[email protected]](OC)CC(N1CCC[[email protected]@]1([H])[[email protected]](OC)[[email protected]@H](C)C(N[[email protected]](C(O)=O)CC2=CC=CC=C2)=O)=O)C)=O)C(C)C)=O

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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MMAF
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