MedChemExpress - Model R406 free base -841290-80-0
R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].MCE products for research use only. We do not sell to patients.
R406 free base
MCE China：R406 free base
Brand：MedChemExpress (MCE)
Cat. No.HY-11108
CAS：841290-80-0
Purity：99.80%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Shipping：Room temperature in continental US; may vary elsewhere.
Description：R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
In Vitro：R406 inhibits adenosine A3 receptor (IC50=0.081 µM), adenosine transporter (IC50=1.84 µM), and monoamine transporter (IC50=2.74 µM)[1]. R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 µM, respectively[1]. R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells[1].
In Vivo：R406 (5 and 10 mg/kg) shows efficacy in the amelioration of the Arthus reaction and in reducing clinical symptoms in the collagen antibody-induced arthritis (CAIA) and K/BxN models of rheumatoid arthritis (RA). Immune complex (IC)-mediated inflammation is reduced by inhibition of Fc receptor signaling with R406[1].
IC50 & Target：Ki: 30 nM (Syk)[1] IC50: 41 nM (Syk)[1] FLT3[1] IC50: 63 nM (Lyn), 37 nM (Lck)[2] Cellular Effect Cell Line Type Value Description References
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References：
[1]. Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008. [Content Brief]
[2]. Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8. [Content Brief]
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