Buy ADCs MonoMethyl auristatin E/MMAE powder CAS:474645-27-7 for anti-body Research only

Buy ADCs MonoMethyl auristatin E/MMAE powder CAS:474645-27-7 for anti-body Research only

MonoMethyl auristatin E

MonoMethyl auristatin E;MMAE;Vedotin;MonoMethyl auristatin E(MMAE, vedotin);HM-297C-22;MonoMethyl auristatin E (MMAE);N-Methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide;N-Methyl-L-valyl-N-[(1S,2R)-4-[(2S)-2-[(1R,2R)-3-[[(1R,2S)-2-hydroxy-1-methyl-2-phenylethyl]amino]-1-methoxy-2-methyl-3-oxopropyl]-1-pyrrolidinyl]-2-methoxy-1-[(1S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide Monomethyl

CAS:474645-27-7

MF:C39H67N5O7

MW:717.97858

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A Brief Introduction of MMAE(Monomethyl Auristatin E, Vedotin)

What\'s MMAE?

Monomethyl auristatin E (abbr. MMAE, commercial name as Vedotin) is a synthetic antineoplastic agent. It cannot be used as a drug itself due to its high toxicity, normally it is linked to a monoclonal antibody (MAB) which directs it to the cancer cells.

Structure of MMAE:

Please refer to: MMAE | Monomethyl Auristatin E

MMAE is actually desmethyl-auristatin E; that is, the N-terminal amino group has only one methyl substituent instead of two as in auristatin E itself.

Toxicity of MMAE:

IC50 of proliferation/viability of tumor cell lines are in the range of 10-7-10-10 M for MMAF/ MMAE auristatin derivatives.

MMAE mechanism of action:

MMAE inhibits cell division by blocking the polymerisation of tubulin as antimitotic agent in ADCs(Antibody Drug Conjugates).

FDA approved ADCs drugs with MMAE:

Adcetris (brentuximab vedotin) is an ADC comprised of a chimeric anti-CD30 antibody (cAC10) conjugated through interchain disulfide bonds to monomethyl auristatin E (MMAE) via a valine-citrulline dipeptide cleavable linker, with

an average DAR of 4.The FDA approval of Adcetris (brentuximab vedotin, Seattle Genetics) in 2011. Adcetris is an antibody-drug conjugate (ADC) directed to the protein CD30, which is expressed in classical Hodgkin lymphoma (HL) and systemic anaplastic large cell lymphoma (sALCL).

Commercial Availability of MMAE:

MMAE is obtained from total synthesis and now available in the market. ALB Technology Limited is a professional ADCs drugs and linkers supplier. ALB Technology Limited provides ADCs products include

Biological Activity

Monomethyl auristatin E (MMAE, vedotin) is a very potent antimitotic agent that inhibits cell division by blocking the polymerisation of tubulin. [1,2,3] The family of auristatins are synthetic analogues of the antineoplastic natural product Dolastatin 10, ultrapotent cytotoxic microtubule inhibitors that are clinically used as payloads in antibody-drug conjugates. [6][7]

Monomethyl auristatin E or MMAE is 100-1000 times more potent than doxorubicin (Adriamycin/Rubex) and cannot be used as a drug itself. However, as part of an antibody-drug conjugate or ADC, MMAE is linked to a monoclonal antibody (mAb) that recognizes a specific marker expression in cancer cells and directs MMAE to a specific, targeted cancer cell.

The linker linking MMAE to the monoclonal antibody is stable in extracellular fluid, but is cleaved by cathepsin once the antibody-drug-conjugate has bound to the targeted cancer cell antigen and entered the cancer cell, after which the ADC releases the toxic MMAE and activates the potent anti-mitotic mechanism. Antibody-drug conjugates enhance the antitumor effects of antibodies and reduce adverse systemic effects of highly potent cytotoxic agents.[2,3,4,5]

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