AZD 3965 is a potent inhibitor of monocarboxylate transporter 1 (MCT1; Ki = 1.6 nM), killing tumor cells that are reliant on glycolysis by blocking lactate transport. It displays six-fold selectivity for MCT1 over MCT2 and is without effect against MCT4 at 10 μM. AZD 3965 increases intratumor lactate levels and decreases tumor growth in mice bearing COR-L103 small cell lung cancer (SCLC) xenografts. AZD 3965 also enhances radiosensitivity in mice with SCLC xenografts.
