| Identification | Back Directory | [Name]
LY2584702 | [CAS]
1082949-67-4 | [Synonyms]
CS-1752
LY2584702
LY2584702 TsOH
LY2584702 BASE
LY2584702 USP/EP/BP
LY-2584702 (free base)
LY-2584702 free base
(LY2584702)
4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methylimidazol-2-yl]piperidin-1-yl]-1H-pyrazolo
4-[4-[4-[4-Fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine
1H-Pyrazolo[3,4-d]pyrimidine, 4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-1H-imidazol-2-yl]-1-piperidinyl]-
4-[4-[4-[4-fluoro-3-(trifluoromethyl)phenyl]-1-methyl-imidazol-2-yl]-1-piperidyl]-1H-pyrazolo[3,4-d]pyrimidine LY2584702 | [Molecular Formula]
C21H19F4N7 | [MDL Number]
MFCD18633220 | [MOL File]
1082949-67-4.mol | [Molecular Weight]
445.43 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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.2?LYS6K2 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.2?Cell 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) Fenton et al. (2011), Functions and regulation of the 70kDa ribosomal S6 kinases; Int. J. Biochem. Cell Biol., 43 47
2) Li et al. (2010), Bifurcation of insulin signaling pathway in the rat liver: mTORC1 required for stimulation of lipogenesis, but no inhibition of gluconeogenesis; Proc. Natl. Acad. Sci. USA 107 3441 |
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| Company Name: |
D&C Chemicals
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| Tel: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
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