maytansinoid

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

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.

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).

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Zn-DPA-maytansinoid conjugate 1, a small molecule-based immune checkpoint-targeting maytansinoid conjugate, effectively induces sustained tumor growth regression and transforms the tumor microenvironment (TME) into an "inflamed hot tumor" [1].

Maytansinoid B, an ADC cytotoxin, conjugates with antibodies to create antibody-drug conjugates (ADCs). This antimitotic agent binds to tubulin, inhibiting microtubule assembly, and induces G2/M arrest in the cell cycle, leading to apoptosis [1] [2].

Maytansinol (Ansamitocin P-0) inhibits microtubule assembly and causes microtubule disassembly in vitro.

DBCO-PEG4-Ahx-DM1 is a drug-linker conjugate that combines the microtubulin inhibitor DM1 (mertansine), an antibody-conjugatable maytansinoid designed to reduce systemic toxicity and improve tumor-specific delivery, with the linker DBCO-PEG4-Ahx, for developing antibody drug conjugates (ADCs).

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.

Lys-SMCC-DM1 (Lys-Nε-MCC-DM1) is an antibody-drug conjugate (ADC) targeting human epidermal growth factor receptor 2 (HER2). It contains the microtubule polymerization inhibitor DM1 as the active metabolite, which inhibits microtubule polymerization. It is commonly used in breast cancer research.

SMCC-DM1 is a drug-coupler coupler consisting of a potent microtubule disrupter, DM1, and a coupler, SMCC, for the preparation of antibody-drug couplers.

DM4-SMCC, a non-cleavable drug-linker conjugate for antibody-drug conjugates (ADC), leverages the antitumor efficacy of DM4 (an antitubulin agent) through attachment with the SMCC linker, exhibiting antitumor activity[1].

DM4-SPDP, a drug-linker conjugate, integrates the antitubulin agent DM4 with the linker SMCC, facilitating the creation of antibody drug conjugates[1]. Additionally, SPDP serves as a short-chain crosslinker enabling amine-to-sulfhydryl conjugation, leveraging NHS-ester and pyridyldithiol groups to establish cleavable (reducible) disulfide bonds with cysteine sulfhydryls[2][3].

Mal-VC-PAB-DM1, a drug-linker conjugate for antibody-drug conjugates (ADCs), exhibits potent antitumor activity. It incorporates DM1, a potent microtubule-disrupting agent, connected through the ADC linker Mal-VC-PAB [1].

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.

DBA-DM4 is a drug-linker conjugate used in antibody-drug conjugate (ADC) synthesis, combining the tubulin inhibitor DM1 with the SPDP linker [1].

SPP-DM1, a drug-linker conjugate for antibody-drug conjugates (ADC), demonstrates potent antitumor activity. It comprises DM1 (a potent microtubule-disrupting agent) connected through the ADC linker SPP[1].

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.

Sulfo-PDBA-DM4 is a drug-linker conjugate for antibody-drug conjugate (ADC) applications, combining the potent tubulin inhibitor DM4 with the gluthatione-cleavable linker Sulfo-PDBA. This configuration harnesses DM4's cytotoxic potential through Sulfo-PDBA's targeted delivery mechanism.

S-Me-DM4 is an intracellular enzyme S-methylated metabolite of DM4, a maytansinoid with microtubule-depolymerizing properties and potent cytotoxicity, employed as an Antibody-Drug Conjugate (ADC) cytotoxin [1].

HS-(CH2)3CO-L-Ala-D-Ala-L-Ala-NH-CH2-S-(CH2)5-CO-DM is a peptide-cleavable agent-linker conjugate used in antibody-drug conjugates (ADCs), with DM indicating the maytansinoid component [1].