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LY2584702 S6 Kinase inhibitor

Cat.No.S7698

LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM.
LY2584702 S6 Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 445.42

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 445.42 Formula

C21H19F4N7

Storage (From the date of receipt)
CAS No. 1082949-67-4 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 4.44 mg/mL (9.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Mechanism of Action

Targets/IC50/Ki
p70S6K [1]
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. [1]

This compound has significant synergistic effects when combined with EGFR inhibitor or with the mTOR inhibitor. [2]

In vivo

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

References

Applications

Methods Biomarkers Images PMID
Western blot p-rpS6 / rpS6 / p-RPS6KB1 / RPS6KB1 S7698-WB1 28792981

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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

Signaling Pathway Map