LFM-A13LFM-A13
MedChemExpress (MCE)
HY-110002
62004-35-7
99.65%
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Room temperature in continental US
may vary elsewhere.
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
LFM-A13 (100 μM
4 h) inhibits Epo-induced phosphorylation of EpoR, JAK2, BTK, STAT5, and ERK1/2 in R10 cells[2]. LFM-A13 (100 μM
transfection 48 h) inhibits the autophosphorylation of JAK2, Tec and BTK in COS cells without affecting the autophosphorylation of Lyn kinase[2]. LFM-A13 potently inhibits Plx1 with IC50 of 10 μM
also inhibits BRK, BMX, FYN and Met with IC50s of 267, 281, 240 and 215 μM, respectively[3].
LFM-A13 (10 or 50 mg/kg
i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer[3]. FM-A13 (50 mg/kg
tiw
i.p.) attenuates DMBA-induced mammary tumorigenesis in mice by modulating a variety of factors associated with cell cycle, survival and apoptosis[4].
Plx1 10 μM (IC50) PLK3 61 μM (IC50) BRK 267 μM (IC50) BMX 281 μM (IC50) FYN 240 μM (IC50) Met 215 μM (IC50) Btk 2.5 μM (IC50)
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[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]