maytansinoid

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

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].

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.

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).

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.

Mertansine (GMP) refers to the GMP grade reagents of Mertansine. 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.

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.

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].

Tusamitamab ravtansine (SAR-408701) is a DM4-linked anti-CEACAM5 antibody-drug conjugate (ADC) comprising a humanized monoclonal antibody targeting carcinoembryonic antigen-related cell adhesion molecule-5 (CEACAM5) conjugated to a cytotoxic maytansinoid, selectively engaging CEACAM5-positive tumor cells [1].

Izeltabart (IMGC-936) is a Maytansinoid-based Antibody-Drug Conjugate (ADC) that specifically targets ADAM9. It consists of a high-affinity humanized antibody conjugated site-specifically to DM21-C, a linker-payload that combines a microtubule-disrupting Maytansinoid with a stable tripeptide linker, maintaining a drug-to-antibody ratio of approximately 2.0. Izeltabart demonstrates cytotoxicity against ADAM9-expressing human tumor cell lines and possesses significant antitumor efficacy in xenograft tumor models [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].

Indatuximab ravtansine (BT-062) is an antibody-drug conjugate (ADC) (Antibody-Drug Conjugates (ADCs)) that consists of a murine-human chimeric form based on B-B4, which specifically targets CD138, linked via a disulfide bond to the maytansinoid drug DM4. It exhibits antitumor activity.