LFM-A13(LFMA13) 布鲁顿氏酪氨酸激酶(BTK)抑制剂|CAS 244240-24-2（53230ES）

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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