FMK-MEA
目录号 : GC34197
FMK-MEA 是一种有效的选择性 p90 核糖体 S6 激酶 (RSK) 抑制剂。
Cas No.:1414811-15-6
Sample solution is provided at 25 µL, 10mM.
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FMK-MEA is a potent and selective p90 Ribosomal S6 Kinase (RSK) inhibitor.
FMK-MEA is a water-soluble derivative of fmk. FMK-MEA treatment inhibits RSK2 kinase activity in diverse, highly invasive human cancer cell lines including 212LN, M4e, A549, and SKBR3 cells. Treatment with the RSK-specific inhibitor FMK-MEA significantly attenuates RSK2 activity, as assessed by the phosphorylation levels of Ser-386 and the consequent invasive ability of A549 cells[1].
FMK-MEA treatment (80 mg/kg/day for 16 days by intraperitoneal injection) in highly metastatic M4e cell xenograft nude mice results in a significant attenuation of LN metastasis. FMK-MEA treatment has no effect on the tumor size, and the proliferation rate of the primary tumor[1].
[1]. Li D, et al. The prometastatic ribosomal S6 kinase 2-cAMP response element-binding protein (RSK2-CREB) signaling pathway up-regulates the actin-binding protein fascin-1 to promote tumor metastasis. J Biol Chem. 2013 Nov 8;288(45):32528-38.
Animal experiment: | Mice[1]For FMK-MEA treatment, each of the nude mice (athymic nu/nu, female, 4-6 weeks old) are injected with 0.5×106cells/100 μL of PBS submandibular to the mylohyoid muscle. On day 5 after injection, mice are divided into two groups with similar average weights with each group receiving either FMK-MEA or PBS. Each mouse is administered 80 mg/kg of FMK-MEA daily by intraperitoneal injection from 5 days after the xenograft for 16 days total. The control group receives PBS alone on the same schedule. Tumor growth is recorded. Mice are sacrificed after 16 days post drug treatment[1]. |
References: [1]. Li D, et al. The prometastatic ribosomal S6 kinase 2-cAMP response element-binding protein (RSK2-CREB) signaling pathway up-regulates the actin-binding protein fascin-1 to promote tumor metastasis. J Biol Chem. 2013 Nov 8;288(45):32528-38. | |
| Cas No. | 1414811-15-6 | SDF | |
| Canonical SMILES | FCC(C1=C(C2=CC=C(C)C=C2)C3=C(N)N=CN=C3N1CCCNCCOC)=O | ||
| 分子式 | C21H26FN5O2 | 分子量 | 399.46 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5034 mL | 12.5169 mL | 25.0338 mL |
| 5 mM | 0.5007 mL | 2.5034 mL | 5.0068 mL |
| 10 mM | 0.2503 mL | 1.2517 mL | 2.5034 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet