LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models. LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus.
|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.
|Solubility||DMSO 7 mg/mL;Water <1 mg/mL|
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.
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LY2584702 is a selective, ATP-competitive p70 S6 kinase inhibitor with IC50 of 4 nM.
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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.
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