|
|
| | LY2584702 Basic information |
| Product Name: | LY2584702 | | Synonyms: | LY2584702;LY-2584702 (free base);LY2584702 TsOH;4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-imidazol-2-yl]-1-piperidyl]-1H-pyrazolo[3,4-d]pyrimidine LY2584702;4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine;4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1H-pyrazolo;LY2584702 USP/EP/BP;1H-Pyrazolo[3,4-d]pyrimidine, 4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]- | | CAS: | 1082949-67-4 | | MF: | C21H19F4N7 | | MW: | 445.42 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1082949-67-4.mol |  |
| | LY2584702 Chemical Properties |
| storage temp. | RT (des.) | | solubility | Soluble in DMSO (up to 1 mg/ml) or in DMF (up to 3 mg/ml). | | form | solid | | color | Yellow | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. |
| | LY2584702 Usage And Synthesis |
| Description | LYS6K2 (1082949-67-4) is a selective inhibitor of the p70 ribosomal S6 kinase (S6K).1 Blocks the phosphorylation of S6 at concentrations as low as 0.1-0.3 μM with no activity at GSK3β and Erk1/2 at 10 μM.2LYS6K2 is a useful tool to dissect insulin receptor signaling pathways and was employed to show that the action of mTORC1 on SREB P-1c expression is not mediated by S6K.2Cell permeable. | | Uses | LY 2584702 is an orally available inhibitor of p70S6K signalling and potential antineoplastic activity. Used in combination with Erlotinib or Everolimus as an anti-tumor treatment. | | in vivo | LY-2584702 demonstrates significant single-agent efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models at two dose levels of 2.5 mg/kg twice daily (BID) and 12.5 mg/kg BID. LY-2584702 demonstrates statistically significant tumour growth reduction at TMED50 (threshold minimum effective dose 50%) (2.3 mg/kg) and TMED90 (10 mg/kg) in the HCT116 colon carcinoma xenograft model[1]. To examine the role of S6K in vivo, EOMA cells expressing shAkt3 are implanted in nu/nu mice, then treated for 14 days with LY-2584702 or Rapamycin. Analysis of tumors removed after 14 days shows that LY-2584702 inhibits S6 phosphorylation almost as effectively as Rapamycin. Loss of Akt3 increases tumor growth as compared with pLKO. LY-2584702 treatment alone does not significantly affect the growth of pLKO tumors. However, LY-2584702 significantly reduces the growth of tumors with shAkt3[2]. | | IC 50 | p70S6K: 4 nM (IC50) | | References | [1] TIM R. FENTON Ivan T G. Functions and regulation of the 70 kDa ribosomal S6 kinases[J]. International Journal of Biochemistry & Cell Biology, 2011, 43 1: Pages 47-59. DOI:10.1016/j.biocel.2010.09.018
[2] SHIJIE LI Joseph L G Michael S Brown. Bifurcation of insulin signaling pathway in rat liver: mTORC1 required for stimulation of lipogenesis, but not inhibition of gluconeogenesis.[J]. Proceedings of the National Academy of Sciences of the United States of America, 2010, 107 8: 3441-3446. DOI:10.1073/pnas.0914798107 |
| | LY2584702 Preparation Products And Raw materials |
|