|Solubility (25°C) *||In vitro||DMSO||1 mg/mL warmed (2.24 mM)|
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Description||LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.|
|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. |
|Animal Models||U87MG glioblastoma and HCT116 colon carcinoma xenograft models|
|Dosages||12.5 mg/kg BID|
Data from [Data independently produced by , , Oncotarget, 2016, 7(25):38451-38466]
Murine DCs were pretreated with PBS or kinase inhibitors (10 μmol/l) wortmanni LY2584702 2 h prior to nicotine (10−7 mol/l) 12~15 h stimulation. MR expression was determined via western blot analyses (C, F). β-actin was used as an internal control.
Data from [Data independently produced by , , J Immunol, 2016, 197(9):3545-3553]
(A) Flow cytometry for TNF-α and IL-12 p40 intracellular expression and ELISA assays for IL-12p70 and IL-23 in supernatants of untreated or treated cells after 24 h. Results were expressed as pictograms per milliliter (± SD) from four independent experiments, each performed in triplicate. *p < 0.05 versus IFN-γ, **p < 0.01 versus IFN-γ.
Leukotriene B₄ Metabolism and p70S6 Kinase 1 Inhibitors: PF-4708671 but Not LY2584702 Inhibits CYP4F3A and the ω-Oxidation of Leukotriene B₄ In Vitro and In Cellulo. [Archambault AS, et al. PLoS One, 2017, 12(1):e0169804]PubMed: 28068410
Anandamide Suppresses Proinflammatory T Cell Responses In Vitro through Type-1 Cannabinoid Receptor-Mediated mTOR Inhibition in Human Keratinocytes. [Chiurchiù V, et al. J Immunol, 2016, 197(9):3545-3553]PubMed: 27694494
Increased translocation of antigens to endosomes and TLR4 mediated endosomal recruitment of TAP contribute to nicotine augmented cross-presentation. [Wang YY, et al. Oncotarget, 2016, 7(25):38451-38466]PubMed: 27224911
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