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product name YK-4-279


Description: YK-4-279 is a potent inhibitor of EWS-FLI1 binding to RNA helicase A (RHA). YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also specifically inhibits ESFT cell growth and induces apoptosis. YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion.

References: Nat Med. 2009 Jul;15(7):750-6; PLoS One. 2014 Dec 5;9(12):e114260. 



Molecular Weight (MW)

366.20 
Formula

C17H13Cl2NO4 
CAS No.

1037184-44-3 
Storage

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

DMSO: 73 mg/mL (199.3 mM)
Water: <1 mg/mL
Ethanol: 51 mg/mL (139.3 mM) 
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19411814

In Vitro

In vitro activity: YK-4-279 eliminates cyclin D levels by blocking the interaction of EWS-FLI1 with RHA in EWS-FLI1-containing TC32 cells. YK-4-279 also specifically inhibits ESFT cell growth and induces apoptosis. YK-4-279 also inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells, and further decreases cell motility and invasion


Kinase Assay:


Cell Assay

In Vivo In vivo, YK-4-279 (1.5 mg/dose i.p.) inhibits the growth of ESFT xenograft tumors. In mouse model, YK-4-279 selectively prevents prostate cancer growth and metastasis in fusion-positive LNCaP-luc-M6 tumors. 
Animal model Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts 
Formulation & Dosage Dissolved in DMSO; 1.5 mg/dose; i.p. injection
References Nat Med. 2009 Jul;15(7):750-6; PLoS One. 2014 Dec 5;9(12):e114260.  

PP 242

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Author: Sodium channel