Monomethyl auristatin E (MMAE)

Catalog No.S7721

Monomethyl auristatin E (MMAE) Chemical Structure

Molecular Weight(MW): 717.98

Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .

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Biological Activity

Description Monomethyl auristatin E (MMAE) is a synthetic antineoplastic agent, which is linked to a monoclonal antibody (MAB). It is also a microtubule-disrupting agent .
In vitro

When coupled to cAC10, MMAE shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis. [1] When coupled to anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro. [2] When coupled to anti-HER2 antibody, hertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells. [3]

In vivo In the Karpas 299 ALCL model, cAC10-vcMMAE (1 mg/kg, i.v.) induces complete, durable tumor regression, while free MMAE (0.36 mg/kg) doesn’t produce detectable antitumor activity. [1] In mouse xenograft models of NHL, anti–CD79b-vcMMAE (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission. [2]

Protocol

Cell Research:

[1]

+ Expand
  • Cell lines: CD30+ Karpas 299 cells
  • Concentrations: ~1000 ng/mL
  • Incubation Time: 96 h
  • Method:

    Cytotoxicity is measured using Alamar Blue dye reduction assay according to the manufacturer's directions. Briefly, a 40% solution (wt/vol) of Alamar Blue is freshly prepared in complete media just before cultures are added. Ninety-two hours after drug exposure, Alamar Blue solution is added to cells to constitute 10% culture volume. Cells are incubated for 4 hours, and dye reduction is measured on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT).


    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (139.27 mM)
Ethanol 100 mg/mL (139.27 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 717.98
Formula
C39H67N5O7
 
CAS No. 474645-27-7
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04084366 Not yet recruiting Drug: OBI-999 Locally Advanced Solid Tumor OBI Pharma Inc January 15 2020 Phase 1|Phase 2
NCT04042480 Recruiting Drug: SGN-CD228A Cutaneous Melanoma|Pleural Mesothelioma|Breast Cancer|Non-small Cell Lung Cancer|Colorectal Cancer|Pancreatic Ductal Adenocarcinoma Seattle Genetics Inc. September 30 2019 Phase 1
NCT03219333 Recruiting Drug: Enfortumab vedotin Carcinoma Transitional Cell|Urinary Bladder Neoplasms|Urologic Neoplasms|Renal Pelvis Neoplasms|Urothelial Cancer|Ureteral Neoplasms|Urethral Neoplasms Astellas Pharma Global Development Inc.|Seattle Genetics Inc.|Astellas Pharma Inc October 8 2017 Phase 2

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Microtubule Associated Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID