IPI-9119
- Product Name
- IPI-9119
- CAS No.
- 1346564-56-4
- Chemical Name
- IPI-9119
- Synonyms
- IPI-9119;IPI-9119, 10 mM in DMSO;4-(4-(2,6-Difluorophenyl)-N-isopropyl-5-oxo-4,5-dihydro-1H-tetrazole-1-carboxamido)-3-phenoxybenzoic acid;Benzoic acid, 4-[[[4-(2,6-difluorophenyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]carbonyl](1-methylethyl)amino]-3-phenoxy-;castration-resistant,AR-V7,AR-FL,prostate,Inhibitor,LNCaP-95,IPI9119,inhibit,22Rv1,IPI-9119,irreversible,C4-2,LNCaP,orally,Fatty Acid Synthase (FASN),IPI 9119,CRPC,cancer
- CBNumber
- CB53067289
- Molecular Formula
- C24H19F2N5O5
- Formula Weight
- 495.43
- MOL File
- 1346564-56-4.mol
IPI-9119 Property
- Boiling point:
- 577.2±60.0 °C(Predicted)
- Density
- 1.43±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (201.84 mM; Need ultrasonic)
- pka
- 4.11±0.10(Predicted)
- form
- Solid
- color
- White to off-white
- 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
- C(O)(=O)C1=CC=C(N(C(N2C(=O)N(C3=C(F)C=CC=C3F)N=N2)=O)C(C)C)C(OC2=CC=CC=C2)=C1
IPI-9119 Chemical Properties,Usage,Production
Uses
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].
Biological Activity
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].
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].
| 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. |
References
[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.
IPI-9119 Preparation Products And Raw materials
Raw materials
Preparation Products
IPI-9119 Suppliers
- Tel
- +1-781-999-5354; +17819995354
- marketing@targetmol.com
- Country
- United States
- ProdList
- 32435
- Advantage
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- tp@aladdinsci.com
- Country
- United States
- ProdList
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- Advantage
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- Tel
- +1-781-999-5354;
- support@targetmol.com
- Country
- United States
- ProdList
- 39035
- Advantage
- 58