ChemicalBook Product Catalog Biochemical Engineering Inhibitors PI3K / Akt / mTOR S6 Kinase Inhibitors LY2584702

LY2584702

Product NameLY2584702
CAS1082949-67-4
MFC21H19F4N7
MW445.42
EINECS
MOL File1082949-67-4.mol

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.

Safety Information

HS Code

2933998090

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

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