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Submit ReviewLFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). Inhibits recombinant BTK with an IC50 value of 2.5 μM and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μM.
LFM-A13 is also offered as part of the Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
M. Wt | 360 |
Formula | C11H8Br2N2O2 |
Storage | Store at RT |
Purity | ≥98% (HPLC) |
CAS Number | 62004-35-7 |
PubChem ID | 54676905 |
InChI Key | UVSVTDVJQAJIFG-VURMDHGXSA-N |
Smiles | C\C(O)=C(/C#N)C(=O)NC1=C(Br)C=CC(Br)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 36 | 100 |
The following data is based on the product molecular weight 360. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.78 mL | 13.89 mL | 27.78 mL |
5 mM | 0.56 mL | 2.78 mL | 5.56 mL |
10 mM | 0.28 mL | 1.39 mL | 2.78 mL |
50 mM | 0.06 mL | 0.28 mL | 0.56 mL |
References are publications that support the biological activity of the product.
Crosby and Pool (2002) Interaction of Bruton's tyrosine kinase and protein kinase Cθ in platelets. J.Biol.Chem. 277 9958 PMID: 11788586
Mahajan et al (1999) Rational design and synthesis of a novel anti-leukemic agent targeting Bruton's tyrosine kinase (BTK), LFM-A13 [α-cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide]. J.Biol.Chem. 274 9587 PMID: 10092645
Vassilev et al (1999) Bruton's tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex. J.Biol.Chem. 274 1646 PMID: 9880544
If you know of a relevant reference for LFM-A13, please let us know.
Keywords: LFM-A13, LFM-A13 supplier, Potent, selective, BTK, inhibitors, inhibits, Brutons, Tyrosine, Kinases, LFMA13, Kinase, (BTK), 1300, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for LFM-A13 include:
Tankiewicz-Kwedlo et al (2018) Erythropoietin Intensifies the Proapoptotic Activity of LFM-A13 in Cells and in a Mouse Model of Colorectal Cancer. Int J Mol Sci 19 PMID: 29690619
He et al (2016) NEK7 is an essential mediator of NLRP3 activation downstream of potassium efflux. Nature 530 354 PMID: 26814970
Colmers and Bains (2018) Balancing tonic and phasic inhibition in hypothalamic CRH-releasing hormone neurons. J Physiol 596 1919 PMID: 29419884
Hart et al (2011) Essential role of Stat3 in PI3K-induced oncogenic transformation. Pain 108 13247 PMID: 21788516
Do you know of a great paper that uses LFM-A13 from Tocris? Please let us know.
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