LP-261 shows potent G2/M block activity in multiple cell lines and exhibits a range of activity from 0.01μM to 0.38 μM across the tested cell lines, the IC50 values for MCF-7, H522, Jurkat, SW-620, BXPC-3, and PC-3 values are 0.01 μM, 0.01 μM, 0.02 μM, 0.05 μM, 0.05μM and 0.07 μM, respectively.
LP-261 exhibits low micromolar potency in the tubulin polymerization assay, the EC50 value of LP-261 is 5.0 μM. LP-261 has the ability to compete with colchicine for binding to tubulin in a [H]colchicine competition binding assay, the EC50 (3.2 μM) for LP-261 to inhibit the binding with a potency similar to that of colchicine itself, and it exhibits a 79% inhibition at a conctration of 30 μM.