| Description | LY2584702 is a selective, ATP-competitive p70S6K inhibitor(IC50: 4 nM). |
| In vitro | In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM[1]. Combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus, LY2584702 has significant synergistic effects [2]. |
| In vivo | LY2584702 (12.5 mg/kg BID), shows significant antitumor activity in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models. [1] |
| Target activity | p70 S6K:4 nM |
| molecular weight | 445.42 |
| Molecular formula | C21H19F4N7 |
| CAS | 1082949-67-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 1 mg/mL(2.24 mM), Heating is recommended. |
| References | 1. Hollebecque A, Houédé N, Cohen EE, Massard C, Italiano A, Westwood P, Bumgardner W, Miller J, Brail LH, Benhadji KA, Soria JC. 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 Mar;50(5):876-84. doi: 10.1016/j.ejca.2013.12.006. Epub 2014 Jan 20. 2. Hollebecque A , Houédé, Nadine, Cohen E E W , et al. A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.[J]. European Journal of Cancer, 2014, 50(5):876-884. |