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 | CC(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.
| 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
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
Keywords: LFM-A13, supplier, Potent, selective, BTK, inhibitors, inhibits, Brutons, Tyrosine, Kinases, LFMA13, Brutons, Tyrosine, Kinase, (BTK), Brutons, Tyrosine, Kinase, (BTK), Tocris Bioscience
