IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC 50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models In Vitro IPI-9119 inhibits FASN in cellular occupancy assays (IC 50 ∼10nM), and shows more than 400-fold selectivity against several additional serine hydrolases. IPI-9119 (0.1-0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest, apoptosis. IPI-9119 (0.05-5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Prostate cancer (PCa) cells (AD LNCaP, AI C4-2, LNCaP-95 and 22Rv1 AI cells) Concentration: 0.1, 0.5 μM Incubation Time: 6 days Result: Inhibited PCa cell growth. Had no growth inhibition in FASN KO PCa cells. Cell Cycle AnalysisCell Line: PCa cells Concentration: 0.1, 0.5 μM Incubation Time: 6 days Result: Reduced the proportion of S-phase cells and increased that of G0/G1-, sub-G1–phase cells and decreased expression of cyclin A2. Western Blot AnalysisCell Line: PCa cells Concentration: 0.05, 0.1, 0.25, 0.5, 5 μM Incubation Time: 6 days Result: Significantly decreased AR-FL protein levels in AD LNCaP, AI C4-2 cells (expressing only AR-FL) and reduced the expression of AR-V7 in LNCaP-95, 22Rv1 AI cells driven by this variant. In Vivo IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 8-10-week male Ncr Nu Castrated mice or castrated NOD male SCID with 22Rv1 or LNCaP-95 cells Dosage: 100 mg/mL Administration: SC pump infusion (0.5 μL/h; 100 mg/mL); for 28 days Result: Inhibited tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models. IC50& Target:IC50: 0.3 nM (FASN)
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IPI-9119
CAS number：1346564-56-4(DMSO) molecular formula：C24H19F2N5O5
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1346564-56-4(DMSO) | molecular formula | C24H19F2N5O5 |
| molecular weight | 495.43 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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