MTX-23 is an AR-based PROTAC. MTX-23 inhibits CaP cellular proliferation by degrading AR-V7 and AR-FL. MTX-23 induces apoptosis.
In Vitro
MTX-23 (compound 16; 0-20 μM; 4 d; 22Rvl cells) inhibits cell growth in dose-dependent manner. MTX-23 (10 μM; 4 d; 22Rvl cells) reduces AR-V7 protein levels. MTX-23 (1 μM; 0-48 h; 22Rvl cells) induces apoptosis and increases annexin-V staining. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: 22Rvl cells Concentration: 0-20 μM Incubation Time: 4 days Result: Reduced the cell count by less than 50 percent. Apoptosis AnalysisCell Line: 22Rvl cells Concentration: 1 μM Incubation Time: 0-48 h Result: Induced cell apoptosis in 22Rvl cells. Western Blot AnalysisCell Line: 22Rvl cells Concentration: 10 μM Incubation Time: 4 days Result: Reduced AR-V7 protein levels.
In Vivo
MTX-23 (compound 16; 2.5 mg/mL; intratumor injection) inhibits tumor growth in nu/nu mice with 22Rvl-Enz R tumor xenografts . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: nu/nu mice with 22Rvl-Enz R tumor xenografts Dosage: 2.5 mg/mL Administration: intratumor injection Result: Inhibited tumor growth in nu/nu mice with 22Rvl-Enz R tumor xenografts.
