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product name LY2584702 Tosylate


Description: LY2584702 Tosylate, also known as LYS6K2,  is a selective, orally available, ATP-competitive p70S6K inhibitor with IC50 of 4 nM. LY2584702 inhibits ribosomal protein S6 Kinase (p70S6K), and prevents phosphorylation of the S6 subunit of ribosomes, thereby inhibiting normal ribosomal function within tumor cells leading to a decrease in protein synthesis and in cellular proliferation. P70S6K is often upregulated in a variety of cancer cells, and is involved in the regulation of cell growth, proliferation, motility, and survival.

References: Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.



Molecular Weight (MW)

617.62
Formula

C28H27F4N7O3S
CAS No.

1082949-68-5
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 7 mg/mL (11.3 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)

 
Synonyms

LYS6K2

other peoduct :

In Vitro

In vitro activity: 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.


Kinase Assay:


Cell Assay:

In Vivo LY2584702 (12.5 mg/kg BID), demonstrates significant antitumor efficacy in both U87MG glioblastoma and HCT116 colon carcinoma xenograft models.
Animal model  
Formulation & Dosage  
References Eur J Cancer. 2014 Mar;50(5):867-75; Eur J Cancer. 2014 Mar;50(5):876-84.

Vatalanib

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Author: Sodium channel