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Cat. No. M6907
LFM-A13 Structure

CAS# 62004-35-7

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Biological Activity

LFM-A13 is a potent and selective inhibitor of Bruton's tyrosine kinase (BTK). LFM-A13 inhibits recombinant BTK with an IC50 value of 2.5 μM and has no activity on other protein kinases ( including JAK1, JAK3, HCK, EGFR kinase and insulin receptor kinase) at concentrations of up to 278 μM. In BCL-1 cells, NALM-6 cells, or normal BALB/c splenocytes, LFM-13 inhibits the enzymatic activity of BTK in BCL-1 cells without affecting the BTK protein expression levels. In human neutrophils, LFM-A13 decreases the tyrosine phosphorylation induced by fMet-Leu-Phe and inhibits the production of superoxide anions and the stimulation of adhesion, chemotaxis, and phospholipase D activity. In vivo, LFM-A13 inhibits osteoclast activity in primary myeloma-bearing SCID-rab mice, prevents myeloma-induced bone resorption and suppresss myeloma growth.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Incubation time
Animal Experiment
Animal models BALB/c mice bearing BCL-1 leukemia
Formulation Suspended in 10% DMSO in PBS
Dosages 50 mg/kg/day, twice daily
Administration i.p.
Chemical Information
Molecular Weight 360.0
Formula C11H8Br2N2O2
CAS Number 244240-24-2
Solubility (25°C) DMSO: ≥ 40 mg/mL warmed
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Bam R, et al. Am J Hematol. Role of Bruton's tyrosine kinase in myeloma cell migration and induction of bone disease.

[2] Frantz, et al. J Med Chem. Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.

[3] Uckun FM, et al. Clin Cancer Res. In vivo pharmacokinetic features, toxicity profile, and chemosensitizing activity of alpha-cyano-beta-hydroxy-beta- methyl-N-(2,5-dibromophenyl)propenamide (LFM-A13), a novel antileukemic agent targeting Bruton's tyrosine kinase.

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Keywords: LFM-A13, CAS# 62004-35-7 supplier, BTK, inhibitors, activators

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