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LFM-A13

CAS No.244240-24-2
Chemical Name:LFM-A13
CBNumber:CB5498231
Molecular Formula:C11H8Br2N2O2
Formula Weight:360
MOL File:244240-24-2.mol

LFM-A13 Property

Melting point 150-151 °C
Boiling point 487.9±45.0 °C(Predicted)
Density 1.909±0.06 g/cm3(Predicted)
storage temp. −20°C
solubility DMSO: 15 mg/mL
form powder
pka 5.20±0.50(Predicted)
color white
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.
UNSPSC Code 12352200
NACRES NA.77

Safety

Hazard Codes :Xn
Risk Statements :20/21/22
Safety Statements :36/37
WGK Germany :3

NFPA 704:

	0
3		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H302+H312+H332
Precautionary statements P261-P264-P280-P301+P312-P302+P352+P312-P304+P340+P312

LFM-A13 Price More Price(1)

Brand: Sigma-Aldrich(India)
Product number: L6920
Product name : LFM-A13
Purity: ≥98% (HPLC), powder
Packaging: 5MG
Price: ₹12849.28
Updated: 2022/06/14
Buy: Buy

LFM-A13 Chemical Properties,Usage,Production

Description 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
Uses LFM-A13 is a potent inhibitor of Polo-like kinase (PLK), used for anti-breast cancer activity. Also a specific Bruton’s tyrosine kinase inhibitor.
in vitro lfm-a13 inhibited recombinant btk expressed in a baculovirus expression vector system. besides its remarkable potency in btk kinase assays, lfm-a13 was also found to be a highly specific inhibitor of btk. even at very high concentrations, lfm-a13 did not affect the activity of other protein tyrosine kinases [1].
in vivo lfm-a13 exhibited a favorable pharmacokinetic behavior which was not adversely affected by the standard chemotherapy drugs and significantly improved the chemotherapy response and survival outcome of bcl-1 leukemia cells challenged mice. while only 14% of mice treated with the standard triple-drug combination treatment became long-term survivors, 41% of mice treated with this combination plus lfm-a13 survived long-term [2].
IC 50 17.2 μm
References 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