AX-0085

AX-0085 is a novel small molecule inhibitor that selectively targets AXL receptor tyrosine kinase, and also acts as an antagonist/inhibitor of EGFR (epidermal growth factor receptor) and IDO1 (indoleamine 2,3-dioxygenase 1). It suppresses AXL/GAS6 signaling, JAK2/STAT1 pathway initiated by interferon-gamma, and downregulates PD-L1 expression, thus reversing T cell exhaustion and immune suppression in tumor microenvironments. AX-0085 is under preclinical and non-clinical investigation for the treatment of cancers characterized by AXL overexpression and is being evaluated primarily in triple-negative breast cancer (TNBC) and non-small cell lung cancer (NSCLC), including osimertinib-resistant forms. In multiple cancer models, AX-0085 effectively inhibits cell proliferation, invasion, EMT, and induces apoptosis by blocking AXL, with a high binding affinity at the ATP binding site. It displays synergistic anti-tumor activity when combined with anti-PD-1 antibody and demonstrates significant anti-tumor effects in both in vitro and in vivo models.[1][3][4][5][6]