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LFM-A13 | BTK inhibitor

CAS:
244240-24-2
Catalog Number:
10-1032
Activity:
BTK inhibitor
Chemical Name:
(2Z)-2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
Molecular Weight:
360
Molecular Formula:
C11H8Br2N2O2
Solubility:
Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 15 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. PROTECT FROM MOISTURE. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

LFM-A13 (244240-24-2) is a selective inhibitor of Bruton’s tyrosine kinase (BTK) – IC50‘s = 2.5 μM (recombinant BTK) and 17.2 μM (human BTK).1,2 It has also been shown to inhibit Polo-like kinase (PLK) – IC50 = 61 μM for human PLK3.3 LFM-A13 displayed no activity (concentrations up to 278 μM) at JAK1, JAK3, HCK, EGFRK and IRK2 or CDK1-3, CHK1, IKK, MAPK1, SAPK2a and ten other tyrosine kinases.3

References/Citations:

1) Vassilev et al. (1999), Bruton’s tyrosine kinase as an inhibitor of the Fas/CD95 death-inducing signaling complex; J. Biol. Chem., 274 1646
2) 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
3) Uckun et al. (2007) Anti-breast cancer activity of LFM-A13, a potent inhibitor of polo-like kinase (PLK); Bioorg. Med. Chem. 15 800

LFM-A13 | BTK inhibitor is also available in the Cellular Metabolism Library.
CAS:
244240-24-2
Catalog Number:
10-1032
Activity:
BTK inhibitor
Chemical Name:
(2Z)-2-Cyano-N-(2,5-dibromophenyl)-3-hydroxy-2-butenamide
Molecular Weight:
360
Molecular Formula:
C11H8Br2N2O2
Solubility:
Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 15 mg/ml).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. PROTECT FROM MOISTURE. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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