CARTProduct Variations
| Product # | Price | Quantity | |
|---|---|---|---|
| VD-GFC-0033-0010-10mg | $90 | ||
| VD-GFC-0033-0050-50mg | $450 |
LFM-A13
$90.00 – $450.00
Product Specification
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Appearance:
Pale brown solid
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CAS Number:
62004-35-7
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Cat.number:
VD-GFC-0033
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Formula:
C11H8Br2N2O2
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MW:
360.0
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Purity:
≥97% by HPLC
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Solubility:
DMSO
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Storage:
+2°C to +8°C. Protect from Light. Packaged under inert gas.
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Synonyms:
Chemical name: α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide
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Size:
10mg, 50mg
Description
A potent and specific inhibitor of Bruton’s Tyrosine Kinase (BTK; IC50 = 17.2 M for human BTK in vitro and IC50 = 2.5 M for recombinant BTK). Also inhibits Polo-like kinase in an ATP-competitive manner (IC50 = 10 M and 61 M 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 M. Enhances the chemosensitivity of BTK-positive B-lineage leukemia cells to ceramide- and vincristine-induced apoptosis. Soluble to 50 mM in EtOH and to 5 mM in 1eq. NaOH.
Mahajan et al (1999) Rational design and synthesis of a novel anti-leukemic agent targeting Bruton’s tyrosine kinase (BTK), LFM-A13 [-cyano--hydroxy--methyl-N-(2,5-dibromophenyl)propenamide]. J.Biol.Chem. 274 9587. Vassilev et al (1999) Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex. J.Biol.Chem. 274 1646. Crosby and Poole (2002) Interaction of Bruton’s tyrosine kinase and protein kinase C in platelets. J.Biol.Chem. 277 9958. 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.
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