In vivo target engagement and tumor LDH activity upon administration of compounds in mice bearing A673 flank xenograft tumors. Mice received a single IV injection of LDHA inhibitors 14, 43, 47, 52, 56, 69, and 71 at 50 mg/kg. At the time of sacrifice, the samples of tumor and plasma were collected and flash-frozen in liquid nitrogen. Compound levels in plasma and tumor were determined by LC–MS/MS, and LDHA activity was measured in tumor lysates.