For research use only. Not for therapeutic Use.
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].
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].
IPI-9119 (SC pump infusion; 0.5 μL/h; 100 mg/mL; for 28 days) inhibits tumor growth of CRPC xenografts mouse models[1].
| Catalog Number | I014804 |
| CAS Number | 1346564-56-4 |
| Synonyms | 4-[[4-(2,6-difluorophenyl)-5-oxotetrazole-1-carbonyl]-propan-2-ylamino]-3-phenoxybenzoic acid |
| Molecular Formula | C24H19F2N5O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H19F2N5O5/c1-14(2)29(19-12-11-15(22(32)33)13-20(19)36-16-7-4-3-5-8-16)23(34)31-24(35)30(27-28-31)21-17(25)9-6-10-18(21)26/h3-14H,1-2H3,(H,32,33) |
| InChIKey | VYXOFKWKPKVNID-UHFFFAOYSA-N |
| SMILES | CC(C)N(C1=C(C=C(C=C1)C(=O)O)OC2=CC=CC=C2)C(=O)N3C(=O)N(N=N3)C4=C(C=CC=C4F)F |
| Reference | [1]. Giorgia Zadra, et al. Inhibition of de novo lipogenesis targets androgen receptor signaling in castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2019 Jan 8;116(2):631-640. [2]. Erin Broph, et al. Abstract 1891: Pharmacological target validation studies of fatty acid synthase in carcinoma using the potent, selective and orally bioavailable inhibitor IPI-9119. |
