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 a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A.

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 a potent tubulin polymerization inhibitor and is used as a antitumor agent. MMAF (Monomethylauristatin F) is widely used as a cytotoxic component of antibody-drug conjugates (ADCs) such as vorsetuzumab mafodotin and SGN-CD19A[1][2][3].

IC50 & Target

Auristatin

 

In Vitro

MMAF inhibits anaplastic large cell lymphoma Karpas 299, breast carcinoma H3396, renal cell carcinoma 786-O and Caki-1 cells with IC50s of 119, 105, 257 and 200 nM in vitro cytotoxicity assay[4].

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[4].

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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Keywords:

MMAFMonomethylauristatin FMicrotubule/TubulinADC CytotoxinInhibitorinhibitorinhibit

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