KGP591, a tubulin polymerization inhibitor with an IC50 of 0.57 µM, effectively induces G2/M arrest, inhibits cell migration, and disrupts microtubule structure and cell morphology in MDA-MB-231 cells. Additionally, it demonstrates antitumor activity in an orthotopic kidney cancer model (RENCA) [1].

KGP591, at a concentration of 100 nM administered for 72 hours, inhibits cell migration and proliferation in MDA-MB-231 cells [1]. At the same concentration but with a 30-minute exposure, KGP591 disrupts the microtubule network in these cells [1]. Furthermore, a higher concentration of 200 nM of KGP591 leads to a G2/M cell cycle arrest after 48 hours of treatment in MDA-MB-231 cells [1].

The prodrug KGP618 of KGP591, at a dose of 150 mg/kg administered subcutaneously for 24 hours, exhibited the efficacy of a tumor-selective vascular disrupting agent (VDA) in a RENCA-luc xenograft BALB/c mouse model [1].