LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation.LY2584702 exhibited anti-tumour activity in preclinical analysis.
|Source||PLoS One (2017). Figure 1. LY2584702|
|Method||Isolation of human neutrophils and cell stimulations|
|Cell Lines||human neutrophils cell|
|Incubation Time||5 minutes|
|Results||This led to a decrease in 20-OH- and 20-COOH-LTB4 levels, and an increase in LTB4 levels. In contrast, LY2584702 did not prevent the metabolism of LTB4 into 20-OH- and 20-COOH-LTB4 in thapsigargin-stimulated neutrophils|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
A phase Ib trial of LY2584702 tosylate, a p70 S6 inhibitor, in combination with erlotinib or everolimus in patients with solid tumours.
Hollebecque A, et al. Eur J Cancer. 2014 Mar;50(5):876-84. PMID: 24456794.
A phase I trial of LY2584702 tosylate, a p70 S6 kinase inhibitor, in patients with advanced solid tumours.
Tolcher A, et al. Eur J Cancer. 2014 Mar;50(5):867-75. PMID: 24440085.
|Related S6 Kinase Products|
LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
SL-0101-1 is a selective p90 RSK inhibitor for RSK2 with IC50 of 89 nM.
FMK is a potent and selective inhibitor of p90 ribosomal protein S6 kinaseRSK2 (wt) with IC50 of 15 nM, >600- and 200-fold selectivity for RSK2 than the C436V and T493M mutants.
PF-4708671 is a novel cell-permeable inhibitor of S6K1 with Ki/IC50 value of 20 nM/160 nM.
BI-D1870 is a small molecule specific inhibitor of the p90 RSK (ribosomal S6 kinase) with an IC50 of 10-30 nM.
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