LFM-A13

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Cat.No. 1300 - LFM-A13 | C11H8Br2N2O2 | CAS No. 62004-35-7
Description: Potent, selective BTK inhibitor
Chemical Name: 2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Literature

Biological Activity

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.

Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 36 100

Preparing Stock Solutions

The following data is based on the product molecular weight 360. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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.

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1 Citation for LFM-A13

Citations are publications that use Tocris products. Selected citations for LFM-A13 include:

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? If so please let us know.

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