Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY 61-3606 dihydrochloride (BAY 61-3606) 是一种口服有效的,ATP 竞争性的,可逆的选择性Syk 抑制剂。它降低神经母细胞瘤细胞中的 ERK1/2 和 Akt 磷酸化,也降低 K-rn 细胞裂解物中 Syk 磷酸化。它作用于乳腺癌细胞,通过下调 Mcl-1 促进 TRAIL 诱导的细胞凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 493 | 现货 | ||
2 mg | ¥ 719 | 现货 | ||
5 mg | ¥ 1,160 | 现货 | ||
10 mg | ¥ 1,950 | 现货 | ||
25 mg | ¥ 3,370 | 现货 | ||
50 mg | ¥ 4,890 | 现货 | ||
100 mg | ¥ 6,860 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,180 | 现货 |
产品描述 | BAY 61-3606 dihydrochloride (BAY 61-3606) is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). |
靶点活性 | Syk:7.5 nM(Ki) |
体外活性 | BAY 61-3606 is a highly selective inhibitor of Syk kinase. Other selected tyrosine kinases, Lyn, Fyn, Src, Itk, and Btk, are not inhibited by BAY 61-3606 in concentrations up to 4.7 μM. BAY 61-3606 is also found to inhibit B cell receptor (BCR)-mediated signaling[1]. Bay 61-3606 is a sensitizer of TRAIL-induced apoptosis. Mcl-1 downregulation by Bay 61-3606 are concentration- and time-dependent in MCF-7 cells. phosphorylation of Syk is reduced by Bay 61-3606 in MCF-7 and T47D cells. Downregulation of Mcl-1 by Bay 61-3606 is independent of Syk in breast cancer cells. Bay 61-3606 promotes the ubiquitin/proteasome-dependent degradation of the Mcl-1 protein in MCF-7 cells. Bay 61-3606 inhibits the phosphorylation of CDK9, RNA polymerase II, and Mcl-1 expression in MCF-7 cells. Bay 61-3606 inhibits CDK9 kinase activity with an in vitro IC50 of 37 nM[2]. |
体内活性 | After 20 days of drug administration, the volume of the xenografted tumor was significantly (P <0.001) reduced the efficacy of Bay 61–3606 when administered in TRAIL combination[2]. Oral administration of BAY 61-3606 to rats significantly suppresses antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema at 3 mg/kg. Furthermore, BAY 61-3606 attenuates antigen-induced airway inflammation in rats[1]. |
激酶实验 | GST-Syk (3.2?ng), 0.5?μg AL, 30?μM ATP, and testing compound in the presence of 0.25% Me2SO are mixed in 50?μL/well of kinase assay buffer in polypropylene U-bottom 96-well microtiter plates. The mixture is incubated for 1?h at room temperature, and the reaction is terminated by the addition of 120?μL of termination buffer. To capture AL, 120?μL of the terminated mixture is transferred to streptavidin-coated plates, followed by incubation at room temperature for more than 30?min. After three ishes with washing buffer, 100?μL of antibody buffer is added and incubated at room temperature for more than 30?min. After three more ishes, 100?μL of enhancement solution is added. Time-resolved fluorescence is measured by multilabel counter ARVO. |
细胞实验 | MCF-7 cells are exposed to TRAIL (indicated concentrations:0, 12.5, 25, 37.5 ng/ml) with or without Bay 61-3606 (2.5 μM) for 24 h; After exposure to the agents for 12 h, MCF-7 cells are subjected to immunocytochemistry using an active Bak antibody; Caspase activity is measured in MCF-7 cells exposed to Bay 61-3606 (5 μM) with or without TRAIL (50 ng/ml) for 24 h.(Only for Reference) |
别名 | BAY 61-3606, BAY-61-3606 dihydrochloride |
分子量 | 463.32 |
分子式 | C20H18N6O3·2HCl |
CAS No. | 648903-57-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 12 mg/mL (25.9 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1583 mL | 10.7917 mL | 21.5834 mL | 53.9584 mL |
5 mM | 0.4317 mL | 2.1583 mL | 4.3167 mL | 10.7917 mL | |
10 mM | 0.2158 mL | 1.0792 mL | 2.1583 mL | 5.3958 mL | |
20 mM | 0.1079 mL | 0.5396 mL | 1.0792 mL | 2.6979 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。
BAY 61-3606 dihydrochloride 648903-57-5 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors Syk BAY 613606 dihydrochloride Spleen tyrosine kinase inhibit Inhibitor BAY-61-3606 BAY 61-3606 BAY-61-3606 Dihydrochloride BAY 61 3606 dihydrochloride BAY-61-3606 dihydrochloride BAY 61-3606 Dihydrochloride inhibitor