ML-230 is an inhibitor of ATP-binding cassette family G member 2 (ABCG2).1 It selectively inhibits JC-1 efflux in Ig-MXP3 cells overexpressing ABCG2 over Jurkat cells overexpressing ABCB1 (IC50s = 0.13 and 4.65 ?M, respectively). ML-230 enhances inhibition of IGROV-1/T8 ovarian cancer cell colony formation induced by topotecan .2 Intratumoral injection of ML-230 (100 nM) and topotecan reduces tumor size in an IGROV-1/T8 mouse xenograft model.
1.Strouse, J.J., Ivnitski-Steele, I., Khawaja, H.M., et al.A selective ATP-binding cassette subfamily G member 2 efflux inhibitor revealed via high-throughput flow cytometryJ. Biomol. Screen.18(1)26-38(2013) 2.Ricci, J.W., Lovato, D.M., Severns, V., et al.Novel ABCG2 antagonists reverse topotecan-mediated chemotherapeutic resistance in ovarian carcinoma xenograftsMol. Cancer Ther.15(12)2853-2862(2016)