microtubule inhibitors

Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research.

Vincristine binds to tubulin and inhibits the formation of microtubules, thereby inhibiting mitosis of the cancer cell. Vincristine can be used as a microtubule-destabilizing agent for research on the treatment of hematologic cancers, such as leukemia and

AMXI-5001 is a potent, orally active inhibitor of PARP1 2 and microtubule aggregation. AMXI-5001 shows selective anti-tumor cytotoxicity against a wide range of human cancer cells with IC50s well below those of existing clinical PARP1 2 inhibitors and induces complete regression of established tumors, including very large ones.

AMXI-5001 hydrochloride is an orally active and potent inhibitor of parp1 2 and microtubule polymerization with significantly lower IC50 values than existing clinical PARP1 2 inhibitors. mxi-5001 hydrochloride exhibits selective antitumor cytotoxicity against a wide range of human cancer cells and is capable of inducing established tumors, including complete regression of larger tumors. including complete regression of larger tumors.

MPT0B098 is a potent microtubule inhibitor through binding to the colchicine-binding site of tubulin. MPT0B098 is active against the growth of various human cancer cells, including chemoresistant cells with IC50 values ranging from 70 to 150 nmol L. MPT0B098 arrests cells in the G2–M phase and subsequently induces cell apoptosis. In addition, MPT0B098 effectively suppresses VEGF-induced cell migration and capillary-like tube formation of HUVECs. Distinguished from other microtubule inhibitors, MPT0B098 not only inhibited the expression levels of HIF-1α protein but also destabilized HIF-1α mRNA. The mechanism of causing unstable of HIF-1α mRNA by MPT0B098 is through decreasing RNA-binding protein, HuR, translocation from the nucleus to the cytoplasm. Notably, MPT0B098 effectively suppresses tumor growth and microvessel density of tumor specimens in vivo. Taken together, our results provide a novel mechanism of inhibiting HIF-1α of a microtubule inhibitor MPT0B098. MPT0B098 is......

Enapotamab vedotin is an investigational antibody-drug conjugate (ADC) specifically targeting the receptor tyrosine kinase AXL. it consists of a monoclonal antibody linked to the potent microtubule-disrupting agent monomethyl auristatin E (MMAE) and demonstrates significant inhibitory potential against high AXL-expressing non-small cell lung cancer (NSCLC), including tumors with resistance to EGFR inhibitors like Osimertinib.