Powder: -20°C for 3 years | In solvent: -80°C for 1 year
R406 free base (R406(free base)) 是一种具有口服活性的,ATP 竞争性的Syk/FLT3抑制剂,Ki 为 30 nM。它有效抑制 Syk 激酶活性,IC50为 41 nM,可减轻免疫复合物介导的炎症。它还抑制 Lyn 和 Lck,IC50分别为 63 nM 和 37 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 413 | 现货 | ||
5 mg | ¥ 663 | 现货 | ||
10 mg | ¥ 1,080 | 现货 | ||
25 mg | ¥ 1,970 | 现货 | ||
50 mg | ¥ 3,570 | 现货 | ||
100 mg | ¥ 5,230 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 687 | 现货 |
产品描述 | R406 free base (R406 (free base)) is a potent Syk inhibitor. |
靶点活性 | Syk:41 nM |
体外活性 | R406口服给药患免疫复合物导致炎症反应的小鼠,明显抑制皮肤反向被动Arthus反应,1 mg/kg和5 mg/kg R406处理,与对照组相比则抑制分别为72%和86%.用10 mg/kg R406处理用胶原抗体处理的小鼠,明显减少炎症和肿胀,将进行性关节炎降低至较低水平,且延迟K/BxN血清转移小鼠模型发病,降低临床关节炎达50%. |
体内活性 | 1 μM或4 μM R406处理DLBCL细胞系,诱导caspases 9和3激活,而不激活caspase 8,导致大部分细胞凋亡。R406在不同细胞中,选择性抑制Syk依赖的信号通路,EC50为33 nM到171 nM,比作用于Syk非依赖性通路效果好很多。R406抑制大型弥漫大B细胞淋巴瘤(DLBCL)细胞系的细胞增殖,EC50值范围为0.8 μM至8.1 μM。R406的预处理在B细胞受体(BCR)交联后完全阻断SYK525/526的磷酸化和R406敏感的DLBCL中SYK依赖性磷酸化BLNK。R406处理24和48小时后,有效降低MMP-9 mRNA水平,比对照组分别降低2.8和4.3倍,并降低RL细胞侵袭能力。 |
激酶实验 | In-vitro Fluorescence Polarization Kinase Assays: R406 is serially diluted in DMSO and then diluted to 1% DMSO in kinase buffer (20 mM HEPES, pH 7.4, 5 mM MgCl2, 2 mM MnCl2, 1 mM DTT, 0.1 mg/mL acetylated BGG). ATP and substrate in kinase buffer are added at room temperature, resulting in a final DMSO concentration on 0.2%. The kinase reactions are performed in a final volume of 20 μL containing 5 μM HS1 peptide substrate and 4 μM ATP and started by addition of 0.125 ng of Syk in kinase buffer. The reaction is allowed to proceed for 40 minutes at room temperature. The reaction is stopped by the addition of 20 μL of PTK quench mix containing EDTA/anti-phosphotyrosine antibody (1X final)/fluorescent phosphopeptide tracer (0.5X final) diluted in FP Dilution Buffer. The plate is incubated for 30 minutes in the dark at room temperature and then read on a Polarion fluorescence polarization plate reader. Data are converted to amount of phosphopeptide present using a calibration curve generated by competition with the phosphopeptide competitor provided in the Tyrosine Kinase Assay Kit. For IC50 determination, R406 is tested at eleven concentrations in duplicate and curve-fitting is performed by non-linear regression analysis using Prism GraphPad Software. |
细胞实验 | DLBCL cell lines are treated with serial dilutions of R406 (0.3, 0.6, 1.25, 2.5, or 5 μM) for 72 or 96 hours. Thereafter, cellular proliferation is determined by MTT assay, and cell apoptosis is assessed by using annexin V–FITC/propidium iodide (PI) staining. For the determination of caspase 9, 8, and 3, cells are lysed, size-fractionated by polyacrylamide gel electrophoresis (PAGE), and immunoblotted. (Only for Reference) |
别名 | R406 (free base) |
分子量 | 470.45 |
分子式 | C22H23FN6O5 |
CAS No. | 841290-80-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 20 mg/mL (42.5 mM)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1256 mL | 10.6281 mL | 21.2562 mL | 53.1406 mL |
5 mM | 0.4251 mL | 2.1256 mL | 4.2512 mL | 10.6281 mL | |
10 mM | 0.2126 mL | 1.0628 mL | 2.1256 mL | 5.3141 mL | |
20 mM | 0.1063 mL | 0.5314 mL | 1.0628 mL | 2.657 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
R406 free base 841290-80-0 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors Syk FLT Inhibitor R406 (free base) FLT3 Cluster of differentiation antigen 135 inhibit R-406 free base CD135 R406 Fms like tyrosine kinase 3 Spleen tyrosine kinase R 406 R-406 inhibitor