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LY2584702 Tosylate S6 Kinase inhibitor

Cat.No.S7704

LY2584702 Tosylate is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.
LY2584702 Tosylate S6 Kinase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 617.62

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Quality Control

Batch: Purity: 99.57%
99.57

Solubility

In vitro
Batch:

DMSO : 7 mg/mL (11.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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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.

Chemical Information, Storage & Stability

Molecular Weight 617.62 Formula

C28H27F4N7O3S

Storage (From the date of receipt)
CAS No. 1082949-68-5 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=CC=C(C=C1)S(=O)(=O)O.CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F

Mechanism of Action

Targets/IC50/Ki
p70S6K
(Cell-free assay)
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. 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.
References

Applications

Methods Biomarkers Images PMID
Western blot p-rpS6 / rpS6 / p-RPS6KB1 / RPS6KB1
S7704-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

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Frequently Asked Questions

Question 1:
What is the difference between S7698 and S7704? i.e, what does the tosylate group do in it?

Answer:
S7704 is the tosylate salt of this compound and S7698 is its free base. 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.

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