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抑制剂/激活剂

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凋亡与自噬

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R406

R406(R406 besylate) 是一种有效的 Syk 抑制剂，无细胞试验中IC50为41 nM，对Syk抑制作用强，但是不抑制Lyn，对Flt3的作用比对Syk低5倍。R406 可诱导凋亡。Phase 1。

货号：
TK0351
规格：

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	841290-81-1
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).
分子式	C22H23N6O5F.C6H6O3S
分子量	628.63
储存条件	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶解性数据	DMSO : ≥ 61 mg/mL (97.04 mM) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)
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.
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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