VPC-14449

VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD) , with IC 50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer In Vitro VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells. VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells (IC 50 =0.34 μM) without affecting AR protein expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration: 0.01, 0.1, 10, 100 μM Incubation Time: 24 hours Result: Suppressed the growth of every tested cell line. Western Blot AnalysisCell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells Concentration: 0.01, 0.1, 10, 100 μM Incubation Time: 24 hours Result: Inhibited endogenous AR transactivation in LNCaP, C4-2 and MR49F cells stimulated with the synthetic androgen R1881. In Vivo VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated Dosage: 100 mg/kg Administration: I.p. twice daily for 4 weeks Result: Suppressed LNCaP tumor volume and blocked serum PSA production. Form:Solid IC50& Target:IC50: 0.34 μM (AR-DBD)

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