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Signaling Pathway

Mc-MMAE

HY-15741

(Maleimidocaproyl-monomethylauristatin E; Mc MMAE; McMMAE)

Mc-MMAE

Mc-MMAE Chemical Structure

Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate; Mc-MMAE is a protective group (maleimidocaproyl) -conjugated MMAE.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $1503 In-stock
1 mg $550 In-stock
5 mg $980 In-stock
10 mg $1500 In-stock
50 mg Get quote
100 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €1473 In-stock
1 mg €539 In-stock
5 mg €960 In-stock
10 mg €1470 In-stock
50 mg Get quote
100 mg Get quote

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Product name: Mc-MMAE
Cat. No.: HY-15741

Mc-MMAE Data Sheet

  • Network Version

    DataSheet

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Related Compound Libraries

Biological Activity of Mc-MMAE

Monomethyl auristatin E (MMAE), a potent tubulin inhibitor, is a toxin payload in antibody drug conjugate; Mc-MMAE is a protective group (maleimidocaproyl) -conjugated MMAE.
IC50 value:
Target:
Effective antibody-drug conjugates (ADC) combine high drug-linker stability in circulation and efficient intratumoral release of drug. Conjugation of monomethyl auristatin E (MMAE) to the anti-CD30 monoclonal antibody (mAb), cAC10, produced a selective and potent ADC against CD30+ anaplastic large cell lymphoma and Hodgkin's disease models. This ADC, cAC10-valine-citrulline-MMAE, uses a protease-sensitive dipeptide linker designed to release MMAE by lysosomal cathepsin B in target cells but maintain a stable linkage and attenuate drug potency in circulation. To evaluate ADC stability in vivo, we developed methods for measuring drug/mAb ratios at progressive times in plasma from ADC-treated mice and nonhuman primates. Anti-idiotype mAb permitted the capture and quantitation of mAb cAC10, whereas antidrug mAb and MMAE-conjugated horseradish peroxidase reporter provided quantitative detection of conjugated drug following its in vitro release by cathepsin B. These data were validated by an alternative ELISA using anti-idiotype and anti-MMAE mAbs for capture and detection, respectively. Both methods differentiated ADC with variable levels of drug loading and were subsequently applied to stability studies in severe combined immunodeficient mice and cynomolgus monkeys. Evaluation of ADC from mouse circulation showed the linker half-life to be ~144 hours (6.0 days), significantly greater than that reported for disulfide- or hydrazone-linked ADCs in mice or human trials. In cynomolgus monkey, the apparent linker half-life was ~230 hours (9.6 days), suggesting that the drug-linker will be highly stable in humans. These data represent the longest reported drug-linker half-life to date and provide the basis for the pronounced specificity and antitumor activity of cAC10-valine-citrulline-MMAE.

Chemical Information

M.Wt 911.18 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C₄₉H₇₈N₆O₁₀
CAS No 863971-24-8
Solvent & Solubility

DMSO: ≥ 51 mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 1.0975 mL 5.4874 mL 10.9748 mL
5 mM 0.2195 mL 1.0975 mL 2.1950 mL
10 mM 0.1097 mL 0.5487 mL 1.0975 mL

References on Mc-MMAE

Inhibitor Kit
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  • 2-Methoxyestradiol

    2-methoxyestradiol (2ME2; NSC-659853) is a natural metabolite of estrogen that is known to inhibit HIF-1 alpha with an IC50 of 0.71 (plusmn) 0.11 (mu)M for the inhibition of BPAEC migration.

  • 4'-Demethylepipodophyllotoxin

    4(acute)-Demethylepipodophyllotoxin(4(acute)-DMEP) is a key intermediate compound for the preparation of podophyllotoxin-type anti-cancer drugs; a potent inhibitor of microtubule assembly.

  • 7-Epi-10-oxo-docetaxel

    7-Epi-10-oxo-docetaxel (Docetaxel Impurity D) is a impurity of docetaxel detected by high performance liquid chromatography (HPLC).

  • 7-Epi-docetaxel

    7-Epi-10-oxo-docetaxel (Docetaxel Impurity C; 7-Epitaxotere) is a impurity of docetaxel.

  • 7-xylosyltaxol

    7-xylosyltaxol(Taxol-7-xyloside) is a taxol (Paclitaxel) derivative; Paclitaxel binds to tubulin and inhibits the disassembly of microtubules.

  • ABT-751

    ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 (mu)M in neuroblastoma and non-neuroblastoma cell lines, respectively.

  • Acetylene-linker-Val-Cit-PABC-MMAE

    Acetylene-linker-Val-Cit-PABC-MMAE consists the ADCs linker (Acetylene-linker-Val-Cit-PABC) and potent tubulin inhibitor (MMAE), Acetylene-linker-Val-Cit-PABC-MMAE is an antibody drug conjugate.

  • Auristatin E

    Auristatin E is a cytotoxic tubulin modifier with potent and selective antitumor activity; MMAE analog and cytotoxin in Antibody-drug conjugates.

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