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Monomethyl auristatin E Chemical Structure
|Product name: Monomethyl auristatin E|
|Cat. No.: HY-15162|
Monomethyl auristatin E (MMAE) is a hot topic in Antibody-drug conjugates (ADCs) studies. It is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin.
IC50 Value: N/A
Target: ADCs cytotoxin; Microtubule/Tubulin
For example VcMMAE, an antibody-drug conjugate (ADC) with potent antitumor activity by using the anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc). Antibody-drug conjugates (ADCs) are designed to combine the exquisite specificity of antibodies to target tumor antigens with the cytotoxic potency of chemotherapeutic drugs. In vivo studies demonstrated that the peptide-linked conjugates induced regressions and cures of established tumor xenografts with therapeutic indices as high as 60-fold. These conjugates illustrate the importance of linker technology, drug potency and conjugation methodology in developing safe and efficacious mAb-drug conjugates for cancer therapy.
|M.Wt||717.98||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO: ≥ 48 mg/mL
|1 mg||5 mg||10 mg|
|1 mM||1.3928 mL||6.9640 mL||13.9280 mL|
|5 mM||0.2786 mL||1.3928 mL||2.7856 mL|
|10 mM||0.1393 mL||0.6964 mL||1.3928 mL|
. Liu, Yuan; Bajjuri, Krishna Mohan; Liu, Cheng; Sinha, Subhash C. Targeting Cell Surface Alpha(v)beta(3) Integrin Increases Therapeutic Efficacies of a Legumain Protease-Activated Auristatin Prodrug. Molecular Pharmaceutics (2012), 9(1), 168-175.
. Bajjuri, Krishna Mohan; Liu, Yuan; Liu, Cheng; Sinha, Subhash C. The Legumain Protease-Activated Auristatin Prodrugs Suppress Tumor Growth and Metastasis without Toxicity. ChemMedChem (2011), 6(1), 54-59.
. Naumovski L, Junutula JR. Glembatumumab vedotin, a conjugate of an anti-glycoprotein non-metastatic melanoma protein B mAb and monomethyl auristatin E for the treatment of melanoma and breast cancer. Curr Opin Mol Ther. 2010 Apr;12(2):248-57.
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