Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PRT-060318 (P142-76) 是一种新颖的、选择性的酪氨酸激酶 (Syk) 抑制剂,其IC50=4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 259 | 现货 | ||
2 mg | ¥ 393 | 现货 | ||
5 mg | ¥ 797 | 现货 | ||
10 mg | ¥ 1,260 | 现货 | ||
25 mg | ¥ 2,520 | 现货 | ||
50 mg | ¥ 3,820 | 现货 | ||
100 mg | ¥ 5,480 | 现货 |
产品描述 | PRT-060318 (P142-76) is a novel selective inhibitor of the Syk tyrosine kinase, as an approach to HIT treatment. |
靶点活性 | Syk:4nM |
体外活性 | PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors[1]. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering[2]. |
体内活性 | In both rabbit and pig models, intravenous infusion of PRT060318 targets maximal inhibition of Syk kinase activity and significantly inhibits arterial thrombosis. The antithrombotic activity of PRT060318 in pigs is remarkable because it was achieved with complete inhibition of CVXN-induced platelet aggregation, with no effect on ADP-induced platelet aggregation, and no prolongation of ear bleeding time[3]. Also, Syk inhibitor PRT318 is an active agent in HIT. Inhibition of Syk signaling with the orally bio-available PRT318 limits the thrombocytopenic and thrombotic effects of HIT IC in vivo[1]. |
细胞实验 | The numbers of cells treated with various doses of PRT318 are followed over time. PRT318 inhibits growth of the sensitive cell lines in a dose-dependent manner. Two sensitive (LY7 and LY18) and 2 resistant (LY3 and LY4) cell lines are treated with indicated doses of PRT318. (Only for Reference) |
别名 | P142-76, PRT318, PRT-060318 2HCl |
分子量 | 340.42 |
分子式 | C18H24N6O |
CAS No. | 1194961-19-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 5.6 mg/mL (16.45 mM), Sonication and heating are recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O | 1 mM | 2.9375 mL | 14.6877 mL | 29.3755 mL | 73.4387 mL |
5 mM | 0.5875 mL | 2.9375 mL | 5.8751 mL | 14.6877 mL | |
10 mM | 0.2938 mL | 1.4688 mL | 2.9375 mL | 7.3439 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。
PRT-060318 1194961-19-7 Angiogenesis Tyrosine Kinase/Adaptors Syk PRT-318 PRT 060318 P142-76 PRT318 PRT-060318 2HCl Inhibitor inhibit PRT 318 Spleen tyrosine kinase PRT060318 inhibitor