FDW028 is an inhibitor of fucosyltransferase 8 (FUC8).[1] It binds to FUC8 (Kd = 5.486 µM) and inhibits core fucosylation in HCT-8 and SW480 colorectal cancer (CRC) cells. FDW028 (50 µM) induces degradation of B7-H3, also known as CD276, via chaperone-mediated autophagy (CMA) in the same cells. In vivo, FDW028 (10 and 20 mg/kg) reduces tumor volume and increases survival in an SW480 mouse xenograft model.
References:
[1].Wang, M., Zhang, Z., Chen, M., et al.FDW028, a novel FUT8 inhibitor, impels lysosomal proteolysis of B7-H3 via chaperone-mediated autophagy pathway and exhibits potent efficacy against metastatic colorectal cancerCell Death Dis.14(8)495(2023).