hemiasterlin analogue E7974

E7974 is a synthetic small molecule analogue of the marine sponge-derived tripeptide hemiasterlin. It acts as an antimitotic and potential antineoplastic agent by binding to the Vinca domain on tubulin, inhibiting tubulin polymerization and microtubule assembly. This leads to depolymerization of existing microtubules, inhibition of mitosis, and suppression of cellular proliferation. Unlike taxanes and vinca alkaloids, E7974 is a poor substrate for the P-glycoprotein (PgP) drug efflux pump, potentially overcoming common mechanisms of drug resistance in cancer therapy. Preclinical studies show that it induces G2-M cell cycle arrest and apoptosis in cancer cells. It has demonstrated broad anti-tumor activity against various human tumor xenografts and has been investigated in phase 1 clinical trials for advanced malignant solid neoplasms and colorectal cancer[1][2][3][5][7].

Other names

hemiasterlin analogue E7974