arq-621

ARQ 621 is a small-molecule allosteric inhibitor of the kinesin-related motor protein Eg5 (also known as KIF11 or kinesin spindle protein). By selectively inhibiting Eg5—a microtubule-based ATPase essential for mitotic spindle assembly—ARQ 621 disrupts mitosis in dividing cells. This leads to G2/M cell cycle arrest and apoptosis in cancer cells. Preclinical studies demonstrated broad-spectrum cytotoxicity against various human cancer cell lines and significant anti-tumor activity in animal models with minimal bone marrow toxicity. A phase I clinical trial was conducted in patients with solid tumors; however, further development appears to have been discontinued[1][3][4][5][6][7].

Other names

Eg5 kinesin-related motor protein inhibitor ARQ 621Eg-5 kinesin-related motor protein inhibitor ARQ 621Eg 5 kinesin-related motor protein inhibitor ARQ 621N-(3-aminopropyl)-3-chloro-N-[(1R)-1-[7-chloro-3,4-dihydro-4-oxo-3-(phenylamino)-2-quinazolinyl]-3-butyn-1-yl]-2-fluorobenzamideUNII-UU55190C8SUNII-UU-55190C8SUNII-UU 55190C8S