| Bioactivity | LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM. LFM-A13 has antiproliferative activity and anticancer activity. LFM-A13 can be used in cancer-related research[1][3][4] | ||||||||||||
| Invitro | LFM-A13 (100 μM; 4 h) 抑制 R10 细胞中 Epo 诱导的 EpoR、JAK2、BTK、STAT5和 ERK1/2 的磷酸化[2]。LFM-A13 (100 μM; 转染 48 h) 抑制 COS 细胞中 JAK2，Tec 和 BTK 的自磷酸化，而不影响 Lyn 激酶自磷酸化[2]。LFM-A13 有效抑制 Plx1，IC50 为 10 μM, 也抑制 BRK、BMX、FYN 和Met，IC50 分别为 267、281、240 和 215 μM[3]。 Cell Proliferation Assay[3] Cell Line: | ||||||||||||
| In Vivo | LFM-A13 (10 或 50 mg/kg; 腹腔注射) 在 MMTV/Neu 转基因小鼠乳腺癌模型中表现出剂量依赖性的抗肿瘤作用[3]。FM-A13 (50 mg/kg; 每周三次; 腹腔注射) 通过调节多种与细胞周期、存活和凋亡相关的因子，可减轻 DMBA 诱导的小鼠乳腺肿瘤发生[4]。 Animal Model: | ||||||||||||
| Name | LFM-A13 | ||||||||||||
| CAS | 62004-35-7 | ||||||||||||
| Formula | C11H8Br2N2O2 | ||||||||||||
| Molar Mass | 360.00 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |