Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CGP 57380 (MNK1 Inhibitor) 是细胞渗透的吡唑-嘧啶类化合物,是一种具有选择性的Mnk1抑制剂,IC50值为 2.2 μM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 295 | 现货 | ||
2 mg | ¥ 433 | 现货 | ||
5 mg | ¥ 713 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,160 | 现货 | ||
50 mg | ¥ 3,220 | 现货 | ||
100 mg | ¥ 4,590 | 现货 | ||
200 mg | ¥ 6,460 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 790 | 现货 |
产品描述 | CGP 57380 (MNK1 Inhibitor) is a potent MNK1 inhibitor with IC50 of 2.2 μM, exhibiting no inhibitory activity on p38, JNK1, ERK1 and -2, PKC, or c-Src-like kinases. |
靶点活性 | MNK1:2.2 μM |
体外活性 | CGP57380 inhibits phosphorylation of eIF4E in vitro with IC50 of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells. [1] CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy. [2] CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs). [3] CGP57380 prevents the serial replating function of BC progenitors. [4] |
体内活性 | CGP57380 (40 mg/kg/d i.p.) potently abrogates the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs. [4] |
激酶实验 | Recombinant p38 isoforms are activated by Mkk6(E) under the following conditions: p38 (100 ng/mL), Mkk6(E) (30 ng/mL), ATP (100 mM) are mixed in kinase buffer (25 mM Hepes, 25 mM b-glycerophosphate, 0.1 mM sodium orthovanadate, 25 mM MgCl2, 2.5 mM DTT, pH 7.4) and incubated for 30 min at 30°C. A typical assay reaction for Mnk1 activity contained Mnk1 (2 ng/mL), HA-eIF4E (10 ng/mL), ATP (300 mM) in kinase buffer. The reaction is started by addition of activated p38 (0.03-3 ng/mL) and stopped after 30 min at 30°C by addition of SDS loading buffer. Inhibitors of Mnk1 are identified under the same assay conditions, except that Mnk1 is pre-activated using active p38a before exposure to the substrate and inhibitors. |
别名 | N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺, MNK1 Inhibitor |
分子量 | 244.23 |
分子式 | C11H9FN6 |
CAS No. | 522629-08-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 45 mg/mL (184.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.0945 mL | 20.4725 mL | 40.945 mL | 102.3625 mL |
5 mM | 0.8189 mL | 4.0945 mL | 8.189 mL | 20.4725 mL | |
10 mM | 0.4095 mL | 2.0473 mL | 4.0945 mL | 10.2363 mL | |
20 mM | 0.2047 mL | 1.0236 mL | 2.0473 mL | 5.1181 mL | |
50 mM | 0.0819 mL | 0.4095 mL | 0.8189 mL | 2.0473 mL | |
100 mM | 0.0409 mL | 0.2047 mL | 0.4095 mL | 1.0236 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。
CGP 57380 522629-08-9 Apoptosis MAPK MNK Mitogen activated protein kinase interacting kinase Inhibitor MAPK interacting kinase inhibit N3-(4-氟苯基)-1H-吡唑并[3,4-D]嘧啶-3,4-二胺 CGP57380 MNK1 Inhibitor MAP kinase interacting kinase CGP-57380 inhibitor