产品说明书
Ralimetinib dimesylate
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同义名 : | - |
| CAS号 : | 862507-23-1 | |
| 货号 : | A413122 | |
| 分子式 : | C26H37FN6O6S2 | |
| 纯度 : | 98% | |
| 分子量 : | 612.737 | |
| MDL号 : | MFCD22572532 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 60 mg/mL(97.92 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 30 mg/mL(48.96 mM) |
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| 动物实验配方： |
PO 0.5% CMC-Na 20 mg/mL suspension |
| 生物活性 | |||
|---|---|---|---|
| 靶点 |
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| 描述 | p38α mitogen-activated protein kinase (MAPK) is activated in cancer cells in response to environmental factors, oncogenic stress, radiation, and chemotherapy. p38α MAPK phosphorylates a number of substrates, including MAPKAP-K2 (MK2), and regulates the production of cytokines in the tumor microenvironment, such as TNF-α, interleukin-1β (IL-1β), IL-6, and CXCL8 (IL-8)[3]. LY2228820 is a novel and effective p38α MAPK inhibitor with an IC50 value of 7 nM in cell free assay. To assess p38α activity in cells more directly, RAW 264.7 cells were treated with LY2228820. It inhibited p38α and the level of pMK2 (phospho-MAPKAP-K2) with IC50s of 7 nM and 34.3 nM, respectively. LY2228820 was orally dosed in Balb/c mice followed by iv LPS administration after 2 h. And the threshold minimum 50% effective dose (TMED50) was less than 1 mg/kg. In the rat CIA (collagen induced arthritis) model, LY2228820 effectively acting on foot swelling, bone erosion, and cartilage destruction, with the TMED50 of 1.5 mg/kg[4]. | ||
| 细胞研究 | |||||
|---|---|---|---|---|---|
| 细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
| A-2780 | 1 μM | Function assay | reduces tumor-driven cord formation | 23335506 | |
| A549 | ~20 μM | Function assay | inhibits LPS-induced CXCL8 production with IC50 of 144.9 nM | 24356814 | |
| CD14+ | ~800 nM | Function assay | inhibits osteoclastogenesis from CD14 positive cells | 18397345 | |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.63mL 0.33mL 0.16mL |
8.16mL 1.63mL 0.82mL |
16.32mL 3.26mL 1.63mL |
| 参考文献 |
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