| Description | LY-2584702 tosylate salt is a selective, ATP-competitive p70S6K inhibitor, used in trials studying the treatment of cancer. |
| 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] LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus. [2] |
| In vivo | LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87 mg glioblastoma and HCT116 colon carcinoma xenograft models. [1] |
| Target activity | p70 S6K:4 nM |
| Synonyms | LY2584702 tosylate |
| molecular weight | 617.62 |
| Molecular formula | C28H27F4N7O3S |
| CAS | 1082949-68-5 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 12 mg/mL (19.43 mM), Sonication is recommended. |
| References | 1. Tolcher A, et al. Eur J Cancer. 2014, 50(5), 867-875. 2. Hollebecque A, et al. Eur J Cancer. 2014, 50(5), 876-884. |
| Citations | 1. Tong M, Wong T L, Zhao H, et al Loss of tyrosine catabolic enzyme HPD promotes glutamine anaplerosis through mTOR signaling in liver cancer. Cell Reports. 2021, 36(8): 109617. 2. Shen S, Wu G, Luo W, et al. Leonurine attenuates angiotensin II-induced cardiac injury and dysfunction via inhibiting MAPK and NF-κB pathway. Phytomedicine. 2022: 154519. 3. Yang N, Zou C, Luo W, et al. Sclareol attenuates angiotensin II‐induced cardiac remodeling and inflammation via inhibiting MAPK signaling. Phytotherapy Research. 2022 4. Lu D, Zhang H, Zhang Y, et al. Secreted MbovP0145 Promotes IL-8 Expression through Its Interactive β-Actin and MAPK Activation and Contributes to Neutrophil Migration. Pathogens 2021, 10, 1628. Pathogens. 2021 5. Shen S, Huang Z, Lin L, et al.Tussilagone attenuates atherosclerosis through inhibiting MAPKs-mediated inflammation in macrophages.International Immunopharmacology.2023, 119: 110066. |