LY-2584702

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Chemical Structure| 1082949-67-4 同义名 : LY-2584702 free base
CAS号 : 1082949-67-4
货号 : A125389
分子式 : C21H19F4N7
纯度 : 99%+
分子量 : 445.416
MDL号 : MFCD18633220
存储条件：

Pure form Keep in dark place,Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(8.98 mM)，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
动物实验配方：
生物活性
描述 LY-2584702 (LY2584702) suppresses the phosphorylation of S6 ribosomal protein (pS6) in HCT116 colon cancer cells, exhibiting an IC50 of 0.1-0.24 μM[1]. The IC50 for inhibiting pS6 in cells is 100 nM. LY-2584702 exhibits activity against S6K-related kinases MSK2 and RSK at higher concentrations (enzyme assay IC50=58-176 nM). In EOMA cells, LY-2584702 dose-dependently inhibits S6K activity, as evidenced by the reduced phosphorylation of the downstream effector S6[2]. LY-2584702 (LY2584702) significantly reduces A549 cell proliferation after 24 h of treatment at 0.1 μM (P<0.05), with more pronounced effects at higher concentrations and/or longer durations. Similarly, in SK-MES-1 cells, a notable decrease is observed with LY-2584702 at 0.6 μM (P<0.05), a concentration significantly higher than that affecting A549[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.23mL

2.25mL

1.12mL

22.45mL

4.49mL

2.25mL
参考文献

[1]Tolcher A, et al. A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumors. Eur J Cancer. 2014 Mar;50(5):867-75.

[2]Phung TL, et al. Akt1 and akt3 exert opposing roles in the regulation of vascular tumor growth. Cancer Res. 2015 Jan 1;75(1):40-50.

[3]Chen B, et al. Hyperphosphorylation of RPS6KB1, rather than overexpression, predicts worse prognosis in non-small cell lung cancer patients. PLoS One. 2017 Aug 9;12(8):e0182891.