SBI-183 is an orally active QSOX1 inhibitor (Kd: 20 μM). It can inhibit the proliferation and invasion phenotypes of renal carcinoma cell lines, triple-negative breast cancer cell lines, lung adenocarcinoma cell lines, and pancreatic ductal adenocarcinoma. In vivo, SBI-183 suppresses tumor growth in two human renal cell carcinoma xenograft mouse models.

SBI-183, administered in concentrations ranging from 6.25 to 50 μmol/L for 15 minutes, inhibits rQSOX1 enzymatic activity in a dose-dependent manner. This compound suppresses the proliferation of tumor cells without affecting fibroblasts or rapidly proliferating PBMCs, at doses of 0.625 to 20 μmol/L over 5 days. It reduces the viability of 786-O, RCJ-41T2, and MDA-MB-231 cells, with IC50 values of 4.6 μM, 3.9 μM, and 2.4 μM, respectively, within a concentration range of 0.076 nM to 40 μM for 72 hours. Additionally, SBI-183, at doses of 2.5 to 20 μM over 4 to 8 days, inhibits tumor invasion in both two-dimensional and three-dimensional models of 786-O, RCJ-41T2, MDA-MB-231, A549, and MIA PaCa2 cells in a dose-dependent manner.

SBI-183 effectively inhibits tumor growth in two human renal cell carcinoma xenograft mouse models, with dosages of 400 μg/mouse/day administered orally for 35 days in the 786-O model, and 100 mg/kg for 21 days in the RCJ-41T2 model.