Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BAY 61-3606 (Syk inhibitor IV) 是一种具有口服活性的,ATP 竞争性的可逆选择性Syk 抑制剂。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。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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 453 | 现货 | ||
2 mg | ¥ 656 | 现货 | ||
5 mg | ¥ 1,310 | 现货 | ||
10 mg | ¥ 2,210 | 现货 | ||
25 mg | ¥ 3,430 | 现货 | ||
50 mg | ¥ 4,980 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,310 | 现货 |
产品描述 | BAY 61-3606 (Syk inhibitor IV) is a potent, ATP-competitive, reversible, and highly selective inhibitor of Syk tyrosine kinase activity (Ki= 7.5 nM), exhibiting no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src. |
体外活性 | BAY61-3606 as an inhibitor of proliferation in colorectal cancer cells expressing mutant forms of K-RAS, but not in isogenic cells expressing wild-type K-RAS. In addition to its anti-proliferative effects in mutant cells, BAY61-3606 exhibited a distinct biological property in wild-type cells in that it conferred sensitivity to inhibition of RAF. In this context, BAY61-3606 acted by inhibiting MAP4K2 (GCK), which normally activates NFκβ signaling in wild-type cells in response to inhibition of RAF. BAY 61-3606 inhibited not only degranulation (IC50 values between 5 and 46 nM) but also lipid mediator and cytokine synthesis in mast cells. BAY 61-3606 was highly efficacious in basophils obtained from healthy human subjects (IC50 = 10 nM) and seems to be at least as potent in basophils obtained from atopic (high serum IgE) subjects (IC50 = 8.1 nM). B cell receptor activation and receptors for Fc portion of IgG signaling in eosinophils and monocytes were also potently suppressed by BAY 61-3606. |
体内活性 | 经口给予大鼠BAY 61-3606,显著抑制了抗原诱导的被动皮肤过敏反应、支气管收缩和支气管水肿,剂量为3 mg/kg。此外,BAY 61-3606还减轻了抗原诱导的大鼠气道炎症。 |
别名 | 2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺, Syk inhibitor IV |
分子量 | 390.4 |
分子式 | C20H18N6O3 |
CAS No. | 732983-37-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 3.9 mg/mL (10 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.5615 mL | 12.8074 mL | 25.6148 mL | 64.0369 mL |
5 mM | 0.5123 mL | 2.5615 mL | 5.123 mL | 12.8074 mL | |
10 mM | 0.2561 mL | 1.2807 mL | 2.5615 mL | 6.4037 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 732983-37-8 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors Syk Spleen tyrosine kinase 2-[[7-(3,4-二甲氧基苯基)咪唑并[1,2-C]嘧啶-5-基]氨基]-3-吡啶甲酰胺 Syk inhibitor IV inhibit BAY 61 3606 Inhibitor BAY 613606 inhibitor