maytansine

Maytansine (NSC-153858), an ansamycin antibiotic originally isolated from the Ethiopian shrub Maytenus serrata, inhibits the assembly of microtubules by binding to tubulin at the rhizoxin binding site.

Maytansine derivative M24 is a drug-linker conjugate used in the production of the antibody-drug conjugate (ADC), specifically ADC REGN5093-M114.

Val-Cit-PAB-MMAE is a molecular entity designed to function as an antibody-drug conjugate (ADC) or as a component of bispecific antigen-binding molecules, specifically targeting the hepatocyte growth factor receptor known as c-Met (MET).

Val-Cit-amide-Cbz-N(Me)-Maytansine, a molecule functioning as both an antibody and a bispecific antigen-binding entity, targets the hepatocyte growth factor receptor c-Met (MET) and is utilized in the formulation of antibody-drug conjugates (ADCs) [1].

DM3-SMe, a maytansine derivative and tubulin inhibitor, acts as the cytotoxic component in antibody-drug conjugates (ADCs). It can bind to antibodies through disulfide bonds or stable thioether bonds and demonstrates high in vitro cytotoxic activity with an IC50 of 0.0011.

DM3 (Maytansinoid DM3) is a maytansine mimic with disulfide or thiol groups, acting as a tubulin inhibitor and serving as the cytotoxic component in antibody-drug conjugates (ADCs).

S-methyl DM1, a thiomethyl derivative of Maytansine, binds to tubulin (Kd of 0.93 μM) and inhibits microtubule polymerization.

Maytansinoid DM4, a thiol-containing maytansine derivative, is a highly potent cytotoxic moiety utilized in ADC applications.

DM1-(PEG)4-DBCO is a drug-linker conjugate that combines the potent microtubulin inhibitor mertansine (DM1) with the DBCO-PEG4-Ahx linker for developing antibody-drug conjugates (ADCs). This conjugation aims to mitigate systemic toxicity associated with maytansine while improving tumor-specific delivery, leveraging DM1's ability as an antibody-conjugatable maytansinoid.

SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugate (ADC) applications, employing the maytansine-based payload DM4 (a tubulin inhibitor) connected through a SPDB linker. This compound demonstrates significant anti-tumor efficacy.

Sulfo-SPDB-DM4 is a drug-linker conjugate designed for antibody-drug conjugates (ADCs) that employs the maytansine-based payload (DM4, an antitubulin agent) connected through the sulfo-SPDB linker.

DM1-SMe (DM1-SSMe) is a potent inhibitor of maytansinoid microtubular. DM1-SMe is about 3 to 10-fold more potent than the parent drug Maytansine, with IC50s of 0.003 to 0.01 nM for DM1-SMe in a panel of human tumor cell lines.

Trastuzumab emtansine (Ado-Trastuzumab emtansine) is an antibody–drug conjugate that combines the HER2-targeted antitumor specificity of trastuzumab with the potent cytotoxic activity of the microtubule inhibitor DM1, Trastuzumab emtansine enables selective intracellular delivery of the cytotoxic payload to HER2-expressing cells and supporting translational and mechanistic research in advanced breast cancer models.

Cantuzumab mertansine (SB-408075; huC242-DM1), an antibody-drug conjugate (ADC), comprises the potent maytansine derivative (DM1) linked to the humanized monoclonal antibody (huC242) targeting CanAg. Demonstrating cytotoxicity against colon cancer cells, this compound shows extensive antitumor effectiveness across various CanAg-positive human tumor xenografts [1] [2].