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LFM-A13

Cat. No. M6907
LFM-A13 Structure
Synonym:

CAS# 62004-35-7

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10mg USD 89.1  USD99 4-7 Days
25mg USD 194.4  USD216 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
Cell Experiment
Cell lines
Preparation method
Concentrations
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 360.0
Formula C11H8Br2N2O2
CAS Number 244240-24-2
Purity >99%
Solubility DMSO: ≥ 40 mg/mL warmed
Storage at -20°C
References

Role of Bruton's tyrosine kinase in myeloma cell migration and induction of bone disease.
Bam R, et al. Am J Hematol. 2013 Jun;88(6):463-71. PMID: 23456977.

Subtlety of the structure-affinity and structure-efficacy relationships around a nonpeptide oxytocin receptor agonist.
Frantz, et al. J Med Chem. 2010;53: 1546. PMID: 20104850.

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.
Uckun FM, et al. Clin Cancer Res. 2002 May;8(5):1224-33. PMID: 12006542.

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  Catalog
Abmole Inhibitor Catalog 2017




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

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