CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor, with an IC50 of 2.6 nM for human CD73. CD73-IN-4 is potential for the research of cancer immunology[1].
CD73-IN-4 (compound 4a) exhibits excellent potency against soluble hCD73 (IC50 = 0.86 nM) and soluble mouse CD73 (mCD73; IC50 = 3.0 nM), CHO cells overexpressing hCD73 (IC50 = 2.6 nM) or mCD73 (IC50 = 13 nM), and the human ovary cancer cell line SKOV-3 (IC50 = 0.55 nM). It exhibits excellent selectivity (IC50 > 10?000 nM) against CD39, A2aR, and NTPDase2, 3, and 8[1].
[1]. Ehesan U Sharif , et al. Discovery of Potent and Selective Methylenephosphonic Acid CD73 Inhibitors. J Med Chem. 2021 Jan 5.