CS 2164

CS 2164 is a multi-kinase inhibitor.¹ It inhibits VEGFR1, -2, and -3 (IC₅₀s = 8, 7, and 9 nM, respectively), PDGFRα and PDGFRβ (IC₅₀s = 1 and 93 nM), c-Kit (IC₅₀ = 4 nM), Aurora B kinase (IC₅₀ = 9 nM), and CSF-1 receptor tyrosine kinase (FMS; IC₅₀ = 7 nM). CS 2164 is selective for these kinases over a panel of 72 additional kinases, 76 GPCRs, two phosphatases, and nine ion channels (IC₅₀s = >100 nM for all). It inhibits VEGF-induced proliferation of human umbilical vein endothelial cells (HUVECs; GI₅₀ = 20.7 nM) and PDGF-induced proliferation of NIH3T3 cells (GI₅₀ = 44.16 nM). In vivo, CS 2164 (20 mg/kg) reduces tumor vascularization and tumor growth in a COLO 320 colon cancer mouse xenograft model. It also reduces tumor volume in A549, HCT-8, SMMC-7721, and MGC803 mouse xenograft models when administered at doses ranging from 2.5 to 40 mg/kg.

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1. Zhou, Y., Shan, S., Li, Z.-B., et al. CS2164, a novel multi-target inhibitor against tumor angiogenesis, mitosis and chronic inflammation with anti-tumor potency. Cancer Sci. 108(3), 469-477 (2017).