产品
编 号：F475076
分子式：C28H29FN6O8S
分子量：628.63
分子式：C28H29FN6O8S
分子量：628.63
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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2mg
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 841290-81-1
产品详情
生物活性：
R406 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 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
体内研究：
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.Animal Model:Female Balb/c mice (6-8 weeks) with CAIA
Dosage:5 and 10 mg/kg
Administration:Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
Result:Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.
Animal Model:Female C57BL/6 mice with arthritis
Dosage:10 mg/kg
Administration:Administered orally one hour before serum injection; b.i.d; for 13 days
Result:Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.
体外研究：
R406 inhibits adenosine A3 receptor (IC50=0.081 μM), adenosine transporter (IC50=1.84 μM), and monoamine transporter (IC50=2.74 μM).?R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 μM, respectively.?R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells.
R406 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 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM).
体内研究：
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.Animal Model:Female Balb/c mice (6-8 weeks) with CAIA
Dosage:5 and 10 mg/kg
Administration:Administered orally, b.i.d, for 14 days, starting 4 hours after antibody challenge on day 0.
Result:Reduced inflammation and swelling, and the arthritis progressed more slowly in treated animals than in vehicle controls.
Animal Model:Female C57BL/6 mice with arthritis
Dosage:10 mg/kg
Administration:Administered orally one hour before serum injection; b.i.d; for 13 days
Result:Delayed the onset and reduced the severity of clinical arthritis. Paw thickening and clinical arthritis were reduced by approximately 50%.
体外研究：
R406 inhibits adenosine A3 receptor (IC50=0.081 μM), adenosine transporter (IC50=1.84 μM), and monoamine transporter (IC50=2.74 μM).?R406 inhibits Huh7 hepatocyte, A549 epithelial, and H1299 lung cancer lines with EC50s of 15.1, 2.9 and 6.3 μM, respectively.?R406 inhibits phosphorylation of Syk substrate LAT in mast cells and BLNK/SLP65 in B cells.
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