LY2584702

LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.

LY2584702 Chemical Structure

LY2584702 Chemical Structure

CAS: 1082949-67-4

Selleck's LY2584702 has been cited by 19 Publications

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Purity & Quality Control

Batch: Purity: 99.02%
99.02

Choose Selective S6 Kinase Inhibitors

Biological Activity

Description LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
Targets
p70S6K [1]
4 nM
In vitro
In vitro

In HCT116 colon cancer cells, LY2584702 inhibits phosphorylation of the S6 ribosomal protein (pS6) with IC50 of 0.1-0.24 μM. [1]

LY2584702 has significant synergistic effects when combined with EGFR inhibitor erlotinib or with the mTOR inhibitor everolimus. [2]

Cell Research Cell lines Neuronal cells
Concentrations 250 nM
Incubation Time 24 h
Method

Cells were treated with indicated concentration of drug for 24 h.

Experimental Result Images Methods Biomarkers Images PMID
Western blot p-rpS6 / rpS6 / p-RPS6KB1 / RPS6KB1 28792981
In Vivo
In vivo

LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models. [1]

Animal Research Animal Models U87MG glioblastoma and HCT116 colon carcinoma xenograft models
Dosages 12.5 mg/kg BID
Administration --
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01241461 Completed Cancer Eli Lilly and Company November 2010 Phase 1
NCT01115803 Terminated Metastases Neoplasm|Carcinoma Non-small Cell Lung|Renal Cell Carcinoma|Neuroendocrine Tumors Eli Lilly and Company March 2010 Phase 1
NCT01394003 Terminated Advanced Cancer Eli Lilly and Company November 2008 Phase 1

Chemical lnformation & Solubility

Molecular Weight 445.42 Formula

C21H19F4N7

CAS No. 1082949-67-4 SDF Download LY2584702 SDF
Smiles CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 4.44 mg/mL ( (9.96 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

Question 1:
what is the difference between S7698 and S7704? Ie., what does the tosylate group do?

Answer:
S7698 is the free base of the compound and S7704 is its tosylate salt. Chemically, salt form is more stable and has a better solubility than free base, however, it also has a higher molecular weight. Biologically, these two forms have the same activities.

S6 Kinase Signaling Pathway Map

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