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LFM-A13 (CAS 244240-24-2) LS-H38

BTK inhibitor, PLK inhibitor
LS-H38-5 / 5 mg / $195
LS-H38-10 / 10 mg / $235
LS-H38-50 / 50 mg / $465
LS-H38-100 / 100 mg / $800
USA Shipment Only
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Description: Bruton's tyrosine kinase (BTK) is a member of the BTK/Tec family of protein tyrosine kinases involved in signal transduction pathways regulating growth and differentiation of B cells. BTK acts as an inhibitor of Fas/APO-1-mediated apoptosis in B cells by preventing FAS-FADD interaction. LFM-A13 is an anti-leukemia agent with apoptosis-promoting and chemosensitizing properties. It acts as an inhibitor of Bruton's tyrosine kinase (BTK) and Polo-like kinase (Plk) with IC50 values of 2.5 µM (mouse recombinant) and 10 µM (Xenopus), respectively. LFM-A13 exhibits minor inhibitory activity against a number of other protein kinases including JAK1, JAK2, EGFR, IRK, IKK, and Cdk1, 2 and 3, as well as several other related kinases. LFM-A13 also exhibits anti-proliferative activity against HER2/Neu-overexpressing breast cancer cells. H38_ChemicalStructureImage.png
2Z-cyano-N-(2,5-dibromophenyl)3-hydroxy-2-butenamide
 
biochemical, chemical, inhibitor
LS-H38
244240-24-2
C11H8Br2N2O2
≥98%
A crystalline solid
 
C/C(=C(\C#N)/C(=O)Nc1cc(Br)ccc1Br)/O
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)/b8-6-
UVSVTDVJQAJIFG-VURMDHGXSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: BTK related products

Usage Information

LFM-A13 is supplied as a crystalline solid. A stock solution may be made by dissolving the LFM-A13 in an organic solvent purged with an inert gas. LFM-A13 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF). The solubility of LFM-A13 in DMSO is approximately 10 mg/ml and approximately 20 mg/ml in DMF. LFM-A13 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, LFM-A13 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. LFM-A13 has a solubility of approximately 0.3 mg/ml in a 1:2 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Vassilev, A., Ozer, Z., Navara, C., et al. Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 deathinducing signaling complex. J. Biol. Chem. 274(3), 1646-1656 (1999).
  2. Mahajan, S., Ghosh, S., Sudbeck, E.A., et al. 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(14), 9587-9599 (1999).
  3. Uckun, F.M., Dibirdik, I., Qazi, S., et al. Anti-breast cancer activity of LFM-A13, a potent inhibitor of pololike kinase (PLK). Biooganic & Medicinal Chemistry 15, 800-814 (2007).

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