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.
|Animal models||BALB/c mice bearing BCL-1 leukemia|
|Formulation||Suspended in 10% DMSO in PBS|
|Dosages||50 mg/kg/day, twice daily|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 40 mg/mL warmed|
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.
|Related BTK Products|
Evobrutinib is a selective BTK inhibitor with an IC50 of 37.9 nM.
BMS-986142 is a potent, selective, reversible BTK inhibitor, shows BTK IC50 = 0.5nM; human WB IC50 = 90 nM.
GDC-0853 is an orally BTK inhibitor with potential antineoplastic activity.
|Btk inhibitor 2
Btk inhibitor 2 (BGB-3111) is a Brutons tyrosine kinase (BTK) inhibitor.
BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.
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