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ADC Toxin Monomethyl auristatin E (MMAE)

ADC Toxin Monomethyl auristatin E (MMAE)

Inquiry
Antimitotic agent used as toxin linked to antibody.
Catalog No. Unit Price Qty
T60001-10s 10 mg solid $369.00

Details

Product Information
Molecular Weight: 717.98
Formula: C39H67N5O7
Purity: ≥95%
CAS#: 474645-27-7
Solubility: DMSO up to 20 mM
Chemical Name: (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide
Storage: Powder: -20oC 1 year

Biological Activity:

Monomethyl auristatin E (MMAE, vedotin) is a very potent anti-mitotic agent that inhibits cell division by blocking the polymerisation of tubulin. Because of ts super toxicity, it cannot be used as a drug itself. In recent cancer therapy developments, it is linked to a monoclonal antibody (mAb) that recognizes a pecific marker expression in cancer cells and directs MMAE to the cancer cells. The linker linking MMAE to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the antibody-drug-conjugate/ADC has bound to the specific cancer cell antigen and entered the cancer cell, thus releasing the oxic MMAE and activating the potent anti-mitotic mechanism.

Reference:

  1. 1. Francisco JA, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. (2003) Blood.102(4):1458-65.
  2. 2. Junutula JR, et al. Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index. (2008) Nat Biotechnol. 26(8):925-32.
  3. 3. Asundi J, et al. An antibody-drug conjugate targeting the endothelin B receptor for the treatment of melanoma. (2011) Clin Cancer Res.17(5):965-75.
  4. 4. Younes A, et al. Results of a Pivotal Phase II Study of Brentuximab Vedotin for Patients With Relapsed or Refractory Hodgkin's Lymphoma. (2012) J Clin Oncol. 30(18):2183-9.
  5. 5. http://en.wikipedia.org/wiki/Monomethyl_auristatin_E


   MMAE_spec.pdf



Products are for research use only. Not for human use.

Description

Details

Product Information
Molecular Weight: 717.98
Formula: C39H67N5O7
Purity: ≥95%
CAS#: 474645-27-7
Solubility: DMSO up to 20 mM
Chemical Name: (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-hydroxy-1-phenylpropan-2-yl)amino)-1-methoxy-2-methyl-3-oxopropyl)pyrrolidin-1-yl)-3-methoxy-5-methyl-1-oxoheptan-4-yl)-N,3-dimethyl-2-((S)-3-methyl-2-(methylamino)butanamido)butanamide
Storage: Powder: -20oC 1 year

Biological Activity:

Monomethyl auristatin E (MMAE, vedotin) is a very potent anti-mitotic agent that inhibits cell division by blocking the polymerisation of tubulin. Because of ts super toxicity, it cannot be used as a drug itself. In recent cancer therapy developments, it is linked to a monoclonal antibody (mAb) that recognizes a pecific marker expression in cancer cells and directs MMAE to the cancer cells. The linker linking MMAE to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the antibody-drug-conjugate/ADC has bound to the specific cancer cell antigen and entered the cancer cell, thus releasing the oxic MMAE and activating the potent anti-mitotic mechanism.

Reference:

  1. 1. Francisco JA, et al. cAC10-vcMMAE, an anti-CD30-monomethyl auristatin E conjugate with potent and selective antitumor activity. (2003) Blood.102(4):1458-65.
  2. 2. Junutula JR, et al. Site-specific conjugation of a cytotoxic drug to an antibody improves the therapeutic index. (2008) Nat Biotechnol. 26(8):925-32.
  3. 3. Asundi J, et al. An antibody-drug conjugate targeting the endothelin B receptor for the treatment of melanoma. (2011) Clin Cancer Res.17(5):965-75.
  4. 4. Younes A, et al. Results of a Pivotal Phase II Study of Brentuximab Vedotin for Patients With Relapsed or Refractory Hodgkin's Lymphoma. (2012) J Clin Oncol. 30(18):2183-9.
  5. 5. http://en.wikipedia.org/wiki/Monomethyl_auristatin_E


   MMAE_spec.pdf



Products are for research use only. Not for human use.

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