(Z)-LFM-A13

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Chemical Structure| 244240-24-2 同义名 : LFM-A13
CAS号 : 244240-24-2
货号 : A147657
分子式 : C11H8Br2N2O2
纯度 : 99%+
分子量 : 360.001
MDL号 : MFCD09878279
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 40 mg/mL(111.11 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BTK

    BTK, Ki:1.4 μM
描述 LFM-A13 significantly reduces BTK activity, with an IC50 value of 17.2 ± 0.8 μM (equivalent to 6.2 ± 0.3 μg/mL). The inhibitory constants (Ki) of LFM-A13 against various kinases, including BTK, JAK1, JAK3, IRK, EGFR, and HCK, have been found to be 1.4 μM, 110 μM, 148 μM, 31.6 μM, 166 μM, and 214 μM, respectively. At a concentration of 200 μM, LFM-A13 notably enhances the susceptibility of ALL-1 cells to apoptosis induced by ceramide[1]. At 100 μM, LFM-A13 impedes Epo-induced phosphorylation of various proteins including EpoR, Jak2, Btk, Stat5, and Erk1/2 in R10 cells. Additionally, at the same concentration, it hinders the auto-phosphorylation of Jak2, Tec, and Btk, but not of Lyn kinase, in COS cells[2]. LFM-A13 exhibits potent inhibition of Plx1 with an IC50 value of 10 μM and demonstrates inhibitory activity against BRK, BMX, and FYN, with IC50 values of 267 μM, 281 μM, 240 μM, and 215 μM, respectively[3].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
BT20 cells 100 μM Function assay Induction of aberrant monopolar and multipolar spindle formation in human BT20 cells assessed as at 100 uM 17098432
PTK1 cells 1 mM Proliferation assay 50 mins Antiproliferative activity against prometaphase PTK1 cells assessed as complete arrest at 1 mM within 50 mins 17098432
Sf21 cells Function assay Inhibition of xenopus recombinant Plx1 expressed in Sf21 cells by measuring autophosphorylation by 15-mins kinase assay, IC50=10.3 μM 17098432
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.89mL

2.78mL

1.39mL

27.78mL

5.56mL

2.78mL
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. Epub 2006 Oct 26.

[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. 2017 Nov 15. "