Mertansine is a potent microtubule-targeted compound that induces mitotic arrest and kills tumor cells at sub-nanomolar concentrations. Mertansine at a concentration of 100 nmol/L suppressed the growth and shortening rates by 35%, quantitatively similarly to the same concentration of vinblastine. Mertansine inhibits the formation of a cross-link between Cys 12 and Cys 201
|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||10 mM in DMSO|
Phase 1/2 Study of the CD56-Targeting Antibody-Drug Conjugate Lorvotuzumab Mertansine (IMGN901) in Combination With Carboplatin/Etoposide in Small-Cell Lung Cancer Patients With Extensive-Stage Disease.
Socinski MA, et al. Clin Lung Cancer. 2017 Jan;18(1):68-76. PMID: 28341109.
Harnessing the Immune System Against Leukemia: Monoclonal Antibodies and Checkpoint Strategies for AML.
Masarova L, et al. Adv Exp Med Biol. 2017;995:73-95. PMID: 28321813.
|Related Microtubule Products|
VcMMAE is a anti-mitotic agent, monomethyl auristatin E (MMAE), linked via the lysosomally cleavable dipeptide, valine-citrulline (vc).
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.
|Ansamitocin P 3
Ansamitocin P-3 is a microtubule inhibitor, it is also a macrocyclic antitumor antibiotic.
Epothilone D is a potent microtubule stabilizer.
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