LFM-A13

LFM-A13 is an inhibitor of Bruton's tyrosine kinase (BTK; IC₅₀ = 2.5 µM).¹ It is selective for BTK over JAK1, JAK3, IRK, EGFR, and HCK (IC₅₀s = >278 µM for all), as well as a panel of seven serine/threonine and 10 tyrosine kinases as well as one lipid kinase (IC₅₀s = >200-500 µM), but does inhibit polo-like kinase 3 (PLK3; K_i = 7.2 µM) and Xenopus PLK1 (Plx1; IC₅₀ = 10 µM).^2,3 LFM-A13 increases anti-FAS antibody-induced apoptosis in NALM-6-UM-1 acute lymphoblastic leukemia (ALL) cells.¹ It reduces tumor growth in an MMTV/neu transgenic mouse model of breast cancer when administered at a dose of 50 mg/kg.³

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1. Vassilev, A., Ozer, Z., Navara, C., et al. Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex. The Journal of Biological Chemisty 274(3), 1646-1656 (1999).

2. Mahajan, S., Ghosh, S., Sudbeck, E.A., et al. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton’s tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide]. The Journal of Biological Chemisty 274(14), 9587-9599 (1999).

3. Uckun, F.M., Dibirdik, I., Qazi, S., et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of polo-like kinase (PLK). Bioorg. Med. Chem. 15(2), 800-814 (2007).