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YK-4-279

Cat. No. M3898
YK-4-279 Structure
Size Price Availability Quantity
10mg USD 85 In stock
50mg USD 300 In stock
100mg USD 540 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

YK-4-279 is a potent inhibitor of ETV1 and inhibits both the primary tumor growth and metastasis of fusion positive prostate cancer xenografts. YK-4-279 inhibits Ewing's sarcoma family tumor (ESFT) cell growth. YK-4-279 induces apoptosis. YK-4-279 validates the splicing mechanism of EWS-FLI1, showing alternatively spliced gene patterns that significantly overlap with EWS-FLI1 reduction and WT human mesenchymal stem cells (hMSC). YK-4-279 inhibits ERG and ETV1 biological activity in fusion-positive prostate cancer cells leading to decreased motility and invasion. Therefore, YK-4-279 may have an impact on metastasis in prostate cancer and it may be further evaluated for its clinical applications in prostate cancer in addition to Ewing's sarcoma.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts
Formulation DMSO
Dosages 1.5 mg/dose
Administration i.p.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 366.2
Formula C17H13Cl2NO4
CAS Number 1037184-44-3
Purity >99%
Solubility DMSO ≥100 mg/mL
Storage at -20°C
References

Oncogenic fusion protein EWS-FLI1 is a network hub that regulates alternative splicing.
Selvanathan SP, et al. Proc Natl Acad Sci U S A. 2015 Mar 3. PMID: 25737553.

A small molecule inhibitor of ETV1, YK-4-279, prevents prostate cancer growth and metastasis in a mouse xenograft model.
Rahim S, et al. PLoS One. 2014 Dec 5;9(12):e114260. PMID: 25479232.

YK-4-279 inhibits ERG and ETV1 mediated prostate cancer cell invasion.
Rahim S, et al. PLoS One. 2011 Apr 29;6(4):e19343. PMID: 21559405.

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  Catalog
Abmole Inhibitor Catalog 2017




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