LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Ribosomal protein S6 kinase 1 inhibitor
Product Description
Information
LY2584702 LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
Targets
p70S6K 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. LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus.
In vivo
LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.
1.Tolcher A, Goldman J, Patnaik A, Papadopoulos KP, Westwood P, Kelly CS, Bumgardner W, Sams L, Geeganage S, Wang T et al.. (2014) A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours.. Eur J Cancer, 50 (5):(867-75). [PMID:24440085]
2.Hollebecque A, Houédé N, Cohen EE, Massard C, Italiano A, Westwood P, Bumgardner W, Miller J, Brail LH, Benhadji KA et al.. (2014) 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, 50 (5):(876-84). [PMID:24456794]
3.Leohr JK, Luffer-Atlas D, Luo MJ, DeBrota DJ, Green C, Mabry TE, Suico JG. (2018) Serum Lipid and Protein Changes in Healthy Dyslipidemic Subjects Given a Selective Inhibitor of p70 S6 Kinase-1.. J Clin Pharmacol, 58 (4):(412-424). [PMID:29178617]
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