LFM-A13 (LFMA13)是一种特异性布鲁顿氏酪氨酸激酶(BTK)抑制剂,可抑制BTK、Plx1和PLK3的活性,IC50分别为2.5 μM、10 μM和61 μM。BTK是B细胞表面受体(BCR)信号通路的关键激酶,调节B细胞的生长、分化,其功能异常被认为和癌症和自体免疫疾病有关。
参考文献
1.Mahajan S, et al. Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [alpha-cyano-beta-hydroxy-beta-methyl-N-(2, 5-dibromophenyl)propenamide]. J Biol Chem. 1999 Apr 2;274(14):9587-99.
2.van den Akker E, et al. The Btk inhibitor LFM-A13 is a potent inhibitor of Jak2 kinase activity. Biol Chem. 2004 May;385(5):409-13.
3.Uckun FM, et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of Polo-like kinase (PLK). Bioorg Med Chem. 2007 Jan 15;15(2):800-14.
4.Sahin K, et al. LFM-A13, a potent inhibitor of polo-like kinase, inhibits breast carcinogenesis by suppressing proliferation activity and inducing apoptosis in breast tumors of mice. Invest New Drugs. 2018 Jun;36(3):388-395.
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