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MMAD

Potent tubulin inhibitor

MMAD

Catalog No. A3630
Size Price Stock
10mg $727.00 Please Inquiry
50mg $1,938.00 Please Inquiry

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Sample solution is provided at 25 µL, 10mM.

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Quality Control & MSDS

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Chemical structure

MMAD

Biological Activity

Description Monomethyl auristatin D (MMAD) is a potent inhibitor of tubulin.
Targets tubulin ADCs toxin        
IC50            

Protocol

Cell experiment:[1]

Preparation method

Soluble in DMSO. Stock solution can be stored at -80℃. Powder can be stored at -20℃ for several years.

Applications

MMAD is a highly potent inhibitor of tubulin [1]. MMAD is one of the auristatins, which are used as the drugs of antibody drug conjugates (ADCs). In ADCs, the therapeutic compounds and the high selectivity of antibodies are combined by the linkers. By taking advantage of antigen-selectivity of MAbs, it can deliver these cytotoxic drugs to antigen-expressing tumor cells, thus increasing both the efficacy and safety of therapy. As a payload of ADCs, MMAD is used to target the tubulin of the tumor cells. It can interfere with tubulin polymerization and induce rapid cell death at low picomolar concentrations [1]. Additionally, MMAD is reported to be used in the production of site-specific antibody drug conjugates (NDCs). In the NDCs, MMAD is combined with anti-5T4 antibody or anti-Her2 antibody. It is shown that the NDCs demonstrate better efficacy and pharmacokinetics [2].

References:

[1] Puja Sapra, Andrea T Hooper, Christopher J, O’Donnell & Hans-Peter Gerber. Investigational antibody drug conjugates for solid tumors. Expert Opin. Investig. Drugs. 2011, 20(8):1131-1149.

[2] Feng Tiana, Yingchun Lu, Anthony Manibusan, Aaron Sellers et al. A general approach to site-specific antibody drug conjugates. PNAS. 2014, February, 111(5): 1766-1771.

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Chemical Properties

Cas No. 203849-91-6 SDF Download SDF
Synonyms Demethyldolastatin 10;Monomethylauristatin D;Monomethyl Dolastatin 10
Canonical SMILES O=C([C@@H]([C@@H](OC)[C@]1([H])CCCN1C(C[C@@H](OC)[C@@H](N(C)C([C@@H](NC([C@H](C(C)C)N([H])C)=O)C(C)C)=O)[C@@H](C)CC)=O)C)N[C@H](C2=NC=CS2)CC3=CC=CC=C3
Formula C41H66N6O6S M.Wt 771.06
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

MMAD is a highly potent inhibitor of tubulin [1].

MMAD is one of the auristatins, which are used as the drugs of antibody drug conjugates (ADCs). In ADCs, the therapeutic compounds and the high selectivity of antibodies are combined by the linkers. By taking advantage of antigen-selectivity of MAbs, it can deliver these cytotoxic drugs to antigen-expressing tumor cells, thus increasing both the efficacy and safety of therapy. As a payload of ADCs, MMAD is used to target the tubulin of the tumor cells. It can interfere with tubulin polymerization and induce rapid cell death at low picomolar concentrations [1].

Additionally, MMAD is reported to be used in the production of site-specific antibody drug conjugates (NDCs). In the NDCs, MMAD is combined with anti-5T4 antibody or anti-Her2 antibody. It is shown that the NDCs demonstrate better efficacy and pharmacokinetics [2].

References:
[1] Puja Sapra, Andrea T Hooper, Christopher J, O’Donnell & Hans-Peter Gerber. Investigational antibody drug conjugates for solid tumors. Expert Opin. Investig. Drugs. 2011, 20(8):1131-1149.
[2] Feng Tiana, Yingchun Lu, Anthony Manibusan, Aaron Sellers et al. A general approach to site-specific antibody drug conjugates. PNAS. 2014, February, 111(5): 1766-1771.