(Z) -LFM-A13

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 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.

Product Specifications

CAS Number

[244240-24-2]

UNSPSC

12352005

Hazard Statement

H302+H312+H332

Target

Btk; JAK; Polo-like Kinase (PLK)

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/z-lfm-a13.html

Purity

99.80

Solubility

DMSO : ≥ 42 mg/mL

Smiles

BrC1=C(NC(/C(C#N)=C(C)\O)=O)C=C(Br)C=C1

Molecular Formula

C11H8Br2N2O2

Molecular Weight

360.01

Precautions

H302+H312+H332

References & Citations

[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]"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. "|[4]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.