X-82

X-82 is a multi-kinase inhibitor.¹ It inhibits VEGFR2, PDGFRβ, FMS-related tyrosine kinase 3 (FLT3), and c-Kit (IC₅₀s = 1.12, 0.13, 0.63, and 0.14 nM, respectively) and is selective for these kinases over RET and AMP-activated kinase α1 (AMPKα1; IC₅₀s = 74.1 and 352.2 nM, respectively). X-82 inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; IC₅₀ = 31 nM).² It decreases VEGF-induced capillary tube formation in HUVECs when used at a concentration of 1 µM and reduces FBS-induced migration of HUVECs at 0.01 or 0.1 µM. In vivo, X-82 (80 mg/kg per day), alone and in combination with the EGFR inhibitor gefitinib (Item No. 13166), reduces tumor volume and growth in an HCC827 non-small cell lung cancer (NSCLC) mouse xenograft model.

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1. Liang, C., Yuan, X., Shen, Z., et al. Vorolanib, a novel tyrosine receptor kinase receptor inhibitor with potent preclinical anti-angiogenic and anti-tumor activity. Mol. Ther. Oncolytics 24, 577-584 (2022).

2. Zhang, K., Wang, L., Wei, A., et al. CM082, a novel angiogenesis inhibitor, enhances the antitumor activity of gefitinib on epidermal growth factor receptor mutant non-small cell lung cancer in vitro and in vivo. Thorac. Cancer 11(6), 1566-1577 (2020).