tcsc1673 Ro3280

Ro3280 is a potent, highly selective inhibitor of PLK1 with an IC₅₀ and a K_d of 3 nM and 0.09 nM, respectively, and nearly has no effect on PLK2 and PLK3.

IC50 & Target: IC50: 3 nM (PLK1)^[1][2]


Kd: 0.09 nM (PLK1), 51 nM (TTK), 84 nM (PTK2)^[2]

In Vitro: Ro3280 (RO3280) inhibits PLK1 activity in NB4 and K562 cells, with an IC₅₀s of 13.45 nM and 301 nM, respectively. RO3280 shows inhibitory activities against the growth of six leukemia cells, with IC₅₀s of 186 nM, 175 nM, 74 nM, 797 nM, 120 nM and 162 nM for U937, HL60, NB4, K562, MV4-11 and CCRF cell lines, respectively. RO3280 also suppresses the growth of primary ALL and AML cells, with IC₅₀s of 35.49-110.76 nM, and 52.80-147.50 nM, respectively. RO3280 (50 or 100 nM) induces apoptosis and cell cycle disorder in acute leukemia cells^[1]. Ro3280 shows potent activity in H82, H69, A549 lung cancer cell lines with EC₅₀s of 6 nM, 7 nM and 82 nM. Ro3280 also inhibits several other cancer cell lines, with low concentration^[2]. RO3280 is cytotoxic to 5637 and T24 human bladder cancer cells, with IC₅₀s of appr 100 nM.

In Vivo: Ro3280 (RO3280, 40 mg/kg, i.v.) inhibits 72% tumor growth in a mouse xenograft model implanted with HT-29 colorectal cancer cells, and when dosed more frequently, RO3280 completely suppresses the tumor growth^[2]. RO3280 (30 mg/kg, once every 5 days, i.p.) shows significant anti-bladder cancer activities in a nude mouse model^[3].