產品描述: LY2584702是一種選擇性的,ATP競爭性的p70S6K抑制劑,IC50為4 nM |
靶點:
p70S6K:4 nM;S6Kinase;?mTOR |
體外研究:
在HCT116結腸癌細胞,LY2584702抑制S6核糖體蛋白質(pS6)的磷酸化,IC50 為0.1-0.24 μM。 LY258470與EGRF抑制劑erlotinib或mTOR抑制劑everolimus結合時,具有顯著的協同效應。 |
體內研究:
LY2584702 (12.5 mg/kg BID),在U87MG 成膠質細胞瘤和HCT116結腸癌異種移植物模型中表現出顯著的抗腫瘤作用 |
細胞實驗:
Cell lines: Neuronal cells Concentrations: 250 nM Incubation Time: 24 h Method: Cells were treated with indicated concentration of drug for 24 h. |
動物實驗:
Animal Models: U87MG 惡性膠質瘤和 HCT116 結腸癌異種移植物模型 Dosages: 12.5 mg/kg BID Administration: -- |
參考文獻:
1. Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours. Eur J Cancer. 2014, 50(5), 867-875. 2. Hollebecque A, et al. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours. Eur J Cancer. 2014, 50(5), 876-884. 3. Park SW, et al. Differential expression of gene co-expression networks related to the mTOR signaling pathway in bipolar disorder. Transl Psychiatry. 2022 May 4;12(1):184. |
溶解性:
soluble in DMSO |
保存條件:
-20℃ |
配置溶液濃度參考:
|
1mg |
5mg |
10mg |
1 mM |
2.245 ml |
11.225 ml |
22.451 ml |
5 mM |
0.449 ml |
2.245 ml |
4.49 ml |
10 mM |
0.225 ml |
1.123 ml |
2.245 ml |
50 mM |
0.045 ml |
0.225 ml |
0.449 ml |
|
注意: |
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