1. Metabolic Enzyme/Protease
  2. Fatty Acid Synthase (FASN)
  3. IPI-9119

IPI-9119 

Cat. No.: HY-124628
Handling Instructions

IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models.

For research use only. We do not sell to patients.

IPI-9119 Chemical Structure

IPI-9119 Chemical Structure

CAS No. : 1346564-56-4

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Description

IPI-9119 is an orally active, selective and irreversible FASN inhibitor with an IC50 of 0.3 nM in vitro biochemical assay. IPI-9119 inhibits tumor growth of castration-resistant prostate cancer (CRPC) xenografts mouse models[1][2].

IC50 & Target

IC50: 0.3 nM (FASN)[1]

In Vitro

IPI-9119 inhibits FASN in cellular occupancy assays (IC50∼10nM), and shows more than 400-fold selectivity against several additional serine hydrolases[2].
IPI-9119 (0.1-0.5 μM; 6 days) inhibits cell growth and induces cell cycle arrest, apoptosis[1].
IPI-9119 (0.05-5 μM; 6 days) inhibits AR-FL and AR-V7 protein expression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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[1]

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.
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[1].

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[1]
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.
Molecular Weight

495.43

Formula

C₂₄H₁₉F₂N₅O₅

CAS No.

1346564-56-4

SMILES

O=C(O)C1=CC=C(N(C(N2N=NN(C3=C(F)C=CC=C3F)C2=O)=O)C(C)C)C(OC4=CC=CC=C4)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

IPI-9119IPI9119IPI 9119Fatty Acid Synthase (FASN)orallyirreversiblecastration-resistantprostatecancerCRPCADLNCaPAIC4-2LNCaP-9522Rv1AR-FLAR-V7Inhibitorinhibitorinhibit

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