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.
|Animal models||Nude mice bearing prostate cancer PC3, TC71 or CHP-100 xenografts|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥100 mg/mL|
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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