IPI-9119

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IPI-9119 是一种口服活性、选择性且不可逆的 FASN 抑制剂 (IC50 = 0.3 nM)。

IPI-9119 is an orally active, selective and irreversible FASN inhibitor (IC50 = 0.3 nM).(In Vitro):IPI-9119 (0.05, 0.1, 0.25, 0.5, 5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression. IPI-9119 (0.1, 0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest and apoptosis. IPI-9119 inhibits FASN in cellular occupancy assays (IC50～10nM) and shows more than 400-fold selectivity against several additional serine hydrolases.(In Vivo):IPI-9119 inhibits tumor growth of castration-resistant prostate cancer in xenografts mouse models.

IPI-9119 inhibits FASN in cellular occupancy assays (IC50～10nM), 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.Cell Viability Assay Cell 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 Analysis Cell 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 Analysis Cell 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.

IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models. 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.

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Metabolic Enzyme/Protease

Fatty Acid Synthase

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1346564-56-4

495.43

C24H19F2N5O5

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (201.84 mM)

N/A

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(-20℃)

With Ice Pack

≥ 2 years