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LY-2584702 tosylate salt

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Chemical Structure| 1082949-68-5 同义名 : LY2584702 Tosylate;LY2584702 (tosylate);LYS6K2
CAS号 : 1082949-68-5
货号 : A137621
分子式 : C28H27F4N7O3S
纯度 : 99%+
分子量 : 617.618
MDL号 : MFCD29054739
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 9 mg/mL(14.57 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

动物实验配方:
生物活性
描述 In the S6K1 enzyme assay, LY-2584702 (LY2584702) demonstrates an IC50 of 2 nM. The IC50 for pS6 inhibition in cells is 100 nM. At higher concentrations, LY-2584702 exhibits activity against S6K-related kinases MSK2 and RSK (enzyme assay IC50=58-176 nM). It dose-dependently reduces S6K activity in EOMA cells, as indicated by decreased phosphorylation of the downstream target S6[2]. LY-2584702 (LY2584702) significantly reduces A549 cell proliferation after 24 hours at a concentration of 0.1 μM (P<0.05), with the decrease becoming more pronounced with extended treatment duration and/or higher drug doses (all P<0.05). Comparable effects are seen in SK-MES-1 cells, though a clear reduction requires LY-2584702 at 0.6 μM (P<0.05), a significantly higher dose than for A549[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.62mL

0.32mL

0.16mL

8.10mL

1.62mL

0.81mL

16.19mL

3.24mL

1.62mL

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.