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LY2584702

Name: LY2584702
Brand: Selleck Chemicals
SKU: S7698
Rating: 5 (16 reviews)

Catalog No.S7698

For research use only.

LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.

CAS No. 1082949-67-4

Selleck's LY2584702 has been cited by 16 publications

Purity & Quality Control

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S6 Kinase Signaling Pathway Map

Biological Activity

Description

LY2584702 is a selective, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. Phase 1.

Targets

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

Assay

Methods	Test Index	PMID

Western blot

p-rpS6 / rpS6 / p-RPS6KB1 / RPS6KB1

28792981

In vivo

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

Protocol (from reference)

Animal Research: ^[1]	Animal Models: U87MG glioblastoma and HCT116 colon carcinoma xenograft models Dosages: 12.5 mg/kg BID Administration: --

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	445.42
Formula	C₂₁H₁₉F₄N₇
CAS No.	1082949-67-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CN1C=C(N=C1C2CCN(CC2)C3=NC=NC4=C3C=NN4)C5=CC(=C(C=C5)F)C(F)(F)F

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In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01241461	Completed	Drug: LY2584702	Cancer	Eli Lilly and Company	November 2010	Phase 1
NCT01115803	Terminated	Drug: LY2584702\|Drug: Erlotinib\|Drug: Everolimus	Metastases Neoplasm\|Carcinoma Non-small Cell Lung\|Renal Cell Carcinoma\|Neuroendocrine Tumors	Eli Lilly and Company	March 2010	Phase 1
NCT01394003	Terminated	Drug: LY2584702	Advanced Cancer	Eli Lilly and Company	November 2008	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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.

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