XL092

XL092 is a multi-kinase inhibitor.¹ It selectively inhibits the receptor tyrosine kinases (RTKs) MET, VEGFR2, Axl, and Mer (IC₅₀s = 3, 15, 5.8, and 0.6 nM, respectively) over serine/threonine kinases for which it has no activity, but does inhibit 28 other RTKs with IC₅₀ values ranging from 3 to 54 nM, as well as additional kinases by greater than 70% at 1 µM. XL092 inhibits the proliferation of SNU-5 human gastric carcinoma cells (IC₅₀ = 98.9 nM), which highly express MET, and human umbilical vein endothelial cells (HUVECs; IC₅₀ = 10.4 nM). It reduces tumor volume and intratumoral MET phosphorylation in NCI H441 human lung cancer and SNU-5 mouse xenograft models when administered at doses of 3 and 10 mg/kg. XL092 (30 mg/kg) increases the number of peripheral B cells and CD4⁺ T cells, and decreases the number of peripheral myeloid cells, in an MC-38 syngeneic mouse model of colon carcinoma, indicating a conversion to an immune-permissive tumor microenvironment.

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1. Hsu, J., Chong, C., Serrill, J., et al. Preclinical characterization of XL092, a novel receptor tyrosine kinase inhibitor of MET, VEGFR2, AXL, and MER. Mol. Cancer Ther. 22(2), 179-191 (2023).