Cirtuvivint

Cirtuvivint is a dual inhibitor of CDC-like kinases (Clks; IC₅₀s = 7.1, 3.6, 30.9, and 4.3 nM for CLK1, -2, -3, and -4, respectively) and dual-specificity tyrosine phosphorylation-regulated kinases (DYRKs; IC₅₀s = 4.7, 22.4, 40.7, and 86.4 nM for DYRK1A, -1B, -2, and -4, respectively).¹ It is selective for these kinases over DYRK3, cyclin-dependent kinase 5 (Cdk5), casein kinase 1ε (CK1ε), and glycogen synthase kinase 3β (GSK3β; IC₅₀s = 2.1, 3.96, 3.02, and >10 µM, respectively). Cirtuvivint reduces the viability of 26 patient-derived tumor cell lines grown as multi-cell type spheroids (IC₉₀s = 0.2-10 µM).¹ It reduces tumor growth in a KG-1a acute myeloid leukemia (AML) mouse xenograft model and reduces tumor volume in an MV4-11 AML mouse xenograft model at 25 mg/kg.²

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1. Lindberg, M.F., Deau, E., Arfwedson, J., et al. Comparative efficacy and selectivity of pharmacological inhibitors of DYRK and CLK protein kinases. J. Med. Chem. 66(6), 4106-4130 (2023).

2. Govindharajulu, J.P., Fluss, S., Hollingshead, M.G., et al. Dynamic switching of apoptosis-modulating bim heterodimers in response to BH₃ Mimetics in xenograft models of hematologic malignancies. Mol. Cancer Ther. 25(9), 1537-1154 (2026).