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

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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

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Hazard and Precautionary Statements (GHS)

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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

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IPI-9119 Suppliers

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1346564-56-4, IPI-9119Related Search:

IPI-9119

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

Benzoic acid, 4-[[[4-(2,6-difluorophenyl)-4,5-dihydro-5-oxo-1H-tetrazol-1-yl]carbonyl](1-methylethyl)amino]-3-phenoxy-

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

1346564-56-4