Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) 是一种口服有效的 MEK 抑制剂,抑制 MEK1 和 MEK2 的 IC50分别为 2 nM。它还能激活自噬,诱导凋亡。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 412 | 现货 | ||
50 mg | ¥ 578 | 现货 | ||
100 mg | ¥ 828 | 现货 | ||
200 mg | ¥ 1,220 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 545 | 现货 |
产品描述 | Trametinib (DMSO solvate) (GSK-1120212 (DMSO solvate)) is a Highly Potent and Selective MEK Inhibitor that specifically inhibits MEK1/2(IC50 :2 nM) |
靶点活性 | MEK1/2:2 nM |
体外活性 | Trametinib DMSO solvate displays remarkable potency in cellular assays for ERK1/2 phosphorylation and growth inhibition and excellent in vivo activity.?Inhibition of the MEK?ERK pathway offers a very promising therapeutic strategy for cancers with activating mutant Ras and Raf, and GSK1120212 (DMSO solvate) has been advanced into phase III trials for advanced or metastatic BRAF mutant melanoma as well as phase I and II studies in subjects with solid tumors or leukemia. |
体内活性 | Trametinib DMSO solvate was then evaluated in vivo in an A549 (KRAS mutant cell line) xenograft model, orally dosing daily for 21 days (qd × 21).Near complete tumor growth inhibition was observed at 5.0 and 2.5 mg/kg [92 and 87% tumor growth inhibition (TGI), respectively] and to a lesser degree at 0.5 and 0.1 mg/kg (62 and 58% TGI).?[Notably, although 5 mg/kg was the maximally tolerated dose (MTD) , 3 mg/kg is the typically observed MTD.] Dose-dependent antitumor activity with GSK1120212 (DMSO solvate) treatment has been similarly reported for several other KRAS and BRAF mutant tumor models. |
别名 | Trametinib DMSO solvate, GSK-1120212 (DMSO solvate), Trametinib dimethyl sulfoxide, JTP-74057 (DMSO solvate) |
分子量 | 693.53 |
分子式 | C28H29FIN5O5S |
CAS No. | 1187431-43-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 69 mg/mL (99.49 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4419 mL | 7.2095 mL | 14.419 mL | 36.0475 mL |
5 mM | 0.2884 mL | 1.4419 mL | 2.8838 mL | 7.2095 mL | |
10 mM | 0.1442 mL | 0.7209 mL | 1.4419 mL | 3.6047 mL | |
20 mM | 0.0721 mL | 0.3605 mL | 0.7209 mL | 1.8024 mL | |
50 mM | 0.0288 mL | 0.1442 mL | 0.2884 mL | 0.7209 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。
Trametinib (DMSO solvate) 1187431-43-1 Apoptosis MAPK MEK Mitogen-activated protein kinase kinase GSK 1120212 JTP 74057 arthritis JTP74057 MAPKK inhibit DMSO solvate Adjuvant-induced orally Trametinib DMSO solvate Inhibitor JTP-74057 GSK-1120212 (DMSO solvate) CIA Trametinib dimethyl sulfoxide JTP-74057 (DMSO solvate) GSK1120212 type collageninduced GSK-1120212 AIA Trametinib MAP2K inhibitor