ABT-869

ABT-869 is a dual VEGFR and PDGFR family kinase inhibitor (IC₅₀s = 0.003, 0.004, 0.004, 0.19, 0.066, 0.003, and 0.014 µM for VEGFR1, VEGFR2, FLT3, VEGFR3, PDGFRβ, CSF-1R, and KIT, respectively).¹ It is selective for these kinases over other tyrosine kinases, including RET, FGFR, Src, EGFR, and c-Met (IC₅₀s = 1.9, >12.5, >50, >50, and >50 µM, respectively), but also inhibits Tie2 (IC₅₀ = 0.17 µM). ABT-869 inhibits the proliferation of HT-29 colon and MDA-MB-435 breast cancer, 9L glioma, and MV4-11 acute myeloid leukemia cells (IC₅₀s = 1.3, 2.4, 0.27, and 0.004 µM, respectively). It induces apoptosis in MV4-11 cells (IC₅₀ = 0.03 µM) and inhibits VEGF-induced uterine edema in mice (ED₅₀ = 0.5 mg/kg).^2,1 ABT-869 (1, 3, and 10 mg/kg) improves survival in a MOLM-13 leukemia mouse xenograft model.²

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1. Albert, D.H., Tapang, P., Magoc, T.J., et al. Preclinical activity of ABT-869, a multitargeted receptor tyrosine kinase inhibitor. Mol. Cancer Ther. 5(4), 995-1006 (2006).

2. Shankar, D.B., Li, J., Tapang, P., et al. ABT-869, a multitargeted receptor tyrosine kinase inhibitor: Inhibition of FLT3 phosphorylation and signaling in acute myeloid leukemia. Blood 109(8), 3400-3408 (2007).