BPR5K230

BPR5K230 is a potent, orally bioavailable, small-molecule dual inhibitor of the receptor tyrosine kinases AXL and MERTK (MER), with IC50 values of 9.2 nM and 4.1 nM, respectively. Developed by the National Health Research Institutes (NHRI) and Academia Sinica in Taiwan, BPR5K230 is designed to target both tumor cells and the tumor immune microenvironment. By simultaneously blocking AXL and MERTK signaling, it suppresses tumor growth, metastasis, and drug resistance (such as sorafenib resistance) while enhancing anti-tumor immune responses by modulating immune cells (e.g., upregulating CD4+ and CD8+ T-cells). BPR5K230 has demonstrated significant in vivo anti-tumor efficacy in various preclinical mouse models, including triple-negative breast cancer (MDA-MB-231, 4T1), colorectal cancer (MC-38), and liver cancer (Hepa 1-6), both as a monotherapy and in combination with immune checkpoint inhibitors like anti-PD-L1 antibodies.