Monomethyl auristatin E (MMAE; Vedotin) is an antimitotic agent which inhibits cell division by blocking the polymerisation of tubulin. 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.
|Cell lines||CD30+ Karpas 299 cells|
|Preparation method||Using Alamar Blue dye reduction assay to measure cytotoxicity according to the manufacturer's directions. Briefly, freshly preparing a 40% solution (wt/vol) of Alamar Blue in complete media just before adding cultures . Ninety-two hours after drug exposure, adding Alamar Blue solution to cells to constitute 10% culture volume. Incubating cells for 4 hours, and measuring dye reduction on a Fusion HT fluorescent plate reader (Packard Instruments, Meriden, CT).|
|Incubation time||96 h|
|Animal models||SCID mice bearing Karpas 299 (ALCL) or L540cy (HD) tumors|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO >100 mg/mL|
|Related Microtubule Products|
Crolibulin (also known as EPC2407 and crinobulin) is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity.
Maytansinol, also known as Ansamitocin P-0, is a potent microtubule depolymerizing agent.
Epothilone D is a potent microtubule stabilizer.
|Estramustine phosphate sodium
Estramustine phosphate sodium is an antimicrotubule chemotherapy agent; arrests prostate cancer cells in the G2/M phase of the cell cycle.
Docetaxel trihydrate(Taxotere trihydrate), an analog of taxol, is an inhibitor of depolymerisation of microtubules through binding to stabilized microtubules.
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