MK-8353
产品说明书
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同义名 : | SCH900353 |
| CAS号 : | 1184173-73-6 | |
| 货号 : | A480964 | |
| 分子式 : | C37H41N9O3S | |
| 纯度 : | 99% | |
| 分子量 : | 691.845 | |
| MDL号 : | N/A | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 105 mg/mL(151.77 mM)，配合低频超声助溶，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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | MK-8353 a highly potent and selective ERK1/2 inhibitor with IC50 values of 20/7nM, possessing good oral bioavailability and anti-tumor efficacy. MK-8353 exhibited anti-proliferative effect on A2058, HT-29 and Colo-205 cells with IC50 values of 371, 51 and 23nM. Oral administration of MK-8353 for 28 days achieved a tumor growth inhibition by 88% at dose of 40mg/kg, BID, and tumor regression by 40% at dose of 60mg/kg, BID, in a Colo-205 human colon xenograft model. MK-8353 caused a dose-proportional decrease in the pERK1/2, and ribosomal S6 kinase (pRSK) proteins, with complete suppression of pERK1 and pERK2 observed at 30 nM MK-8353 in A2058 cells post 24h. | ||
| 作用机制 | MK-8353 is an indazole-pyrrolidine derivative and it can form a complex with ERK, which leads to the inability of MEK to catalyze the phosphorylation of the ERK–MK-8353 complex.[3] | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT01358331 | Tumor, Solid | Phase 1 | Terminated | - | - |
| NCT03745989 | Solid Tumors | Phase 1 | Not yet recruiting | May 6, 2022 | - |
| NCT02972034 | Neoplasms Col... 展开 >>orectal Cancer 收起 << | Phase 1 | Recruiting | October 29, 2021 | United States, Michigan ... 展开 >> Call for Information (Investigational Site 0002) Recruiting Grand Rapids, Michigan, United States, 49546 United States, Tennessee Call for Information (Investigational Site 0001) Recruiting Nashville, Tennessee, United States, 37203 Canada, Quebec Merck Canada Recruiting Kirkland, Quebec, Canada, H9H 4M7 Contact: Medical Information Centre Centre d'information medicale Merck Canada Inc. 514-428-8600 / 1-800-567-2594 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
1.45mL 0.29mL 0.14mL |
7.23mL 1.45mL 0.72mL |
14.45mL 2.89mL 1.45mL |
| 参考文献 |
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