435300
LFM-A13
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s Tyrosine Kinase (BTK; IC₅₀ = 17.2 µM for human BTK in vitro and IC₅₀ = 2.5 µM for recombinant BTK).
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Synonym(s):
LFM-A13, α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide, BTK Inhibitor I, Bruton′s Tyrosine Kinase Inhibitor I
Empirical Formula (Hill Notation):
C11H8Br2N2O2
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Quality Level
Assay
≥97% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
light brown
solubility
DMSO: 200 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C11H8Br2N2O2/c1-6(16)8(5-14)11(17)15-10-4-7(12)2-3-9(10)13/h2-4,16H,1H3,(H,15,17)
InChI key
UVSVTDVJQAJIFG-UHFFFAOYSA-N
General description
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
A potent, cell-permeable, reversible, substrate competitive, and specific inhibitor of Bruton′s tyrosine kinase (BTK; IC50 = 17.2 µM for human BTK in vitro and IC50 = 2.5 µM for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 µM and 61 µM for Plx1 and Plk3, respectively), and displays antitumor properties. Does not affect the enzymatic activity of other protein tyrosine kinases, including EGFR, HCK, IRK JAK1, and JAK3 even at concentrations of 278 µM. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Human Bruton′s Tyrosine Kinase (BTK)
Human Bruton′s Tyrosine Kinase (BTK)
Product competes with ATP.
Reversible: yes
Target IC50: 17.2 µM for human BTK in vitro and 2.5 µM for recombinant BTK
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Uckun, F.M., et al. 2006. Bioorg. Med. Chem. In press.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
Mahajan, S., et al. 1999. J. Biol. Chem. 274, 9587.
Vassilev, A., et al. 1999. J. Biol. Chem. 274, 1646.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 1
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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