DM4 has anticancer properties of maytansinoids due to their ability to disrupt microtubule function. Maytansinoid DM4 can be use to make antibody drug conjugates such as Anetumab ravtansine (BAY 94-9343) and Indatuximab ravtansine (BT062). Maytansinoids inhibit tubulin polymerization and microtubule assembly and enhance microtubule destabilization, so there is potent suppression of microtubule dynamics resulting in a mitotic block and subsequent apoptotic cell death.
|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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 70 mg/mL|
 Ruoping Tang, et al. BMC Cancer. P-gp Activity Is a Critical Resistance Factor Against AVE9633 and DM4 Cytotoxicity in Leukaemia Cell Lines, but Not a Major Mechanism of Chemoresistance in Cells From Acute Myeloid Leukaemia P atl ents.
|Related Microtubule Products|
Tubulysin family are originally isolated from the myxobacteria Archangium geophyra and Angiococcus disciformis, and are potent microtubule destabilizing agents.
Taltobulin hydrochloride (HTI-286 hydrochloride), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
Taltobulin (HTI-286), a synthetic analogue of the tripeptide hemiasterlin, is a potent antimicrotubule agent that circumvents P-glycoprotein-mediated resistance in vitro and in vivo.
MMAF (Monomethylauristatin F) hydrochloride is a potent tubulin polymerization inhibitor and is used as a antitumor agent.
Entasobulin is a β-tubulin polymerization inhibitor with potential anticancer activity.
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