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

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

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 545 In-stock
Solution
10 mM * 1 mL in DMSO USD 545 In-stock
Solid
5 mg USD 500 In-stock
10 mg USD 800 In-stock
25 mg USD 1500 In-stock
50 mg USD 2400 In-stock
100 mg USD 3840 In-stock
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Based on 1 publication(s) in Google Scholar

IPI-9119 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

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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].

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

IPI-9119 Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (201.84 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0184 mL 10.0922 mL 20.1845 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0184 mL 10.0922 mL 20.1845 mL 50.4612 mL
5 mM 0.4037 mL 2.0184 mL 4.0369 mL 10.0922 mL
10 mM 0.2018 mL 1.0092 mL 2.0184 mL 5.0461 mL
15 mM 0.1346 mL 0.6728 mL 1.3456 mL 3.3641 mL
20 mM 0.1009 mL 0.5046 mL 1.0092 mL 2.5231 mL
25 mM 0.0807 mL 0.4037 mL 0.8074 mL 2.0184 mL
30 mM 0.0673 mL 0.3364 mL 0.6728 mL 1.6820 mL
40 mM 0.0505 mL 0.2523 mL 0.5046 mL 1.2615 mL
50 mM 0.0404 mL 0.2018 mL 0.4037 mL 1.0092 mL
60 mM 0.0336 mL 0.1682 mL 0.3364 mL 0.8410 mL
80 mM 0.0252 mL 0.1262 mL 0.2523 mL 0.6308 mL
100 mM 0.0202 mL 0.1009 mL 0.2018 mL 0.5046 mL
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IPI-9119 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

IPI-91191346564-56-4IPI9119IPI 9119Fatty Acid Synthase (FASN)orallyirreversiblecastration-resistantprostatecancerCRPCADLNCaPAIC4-2LNCaP-9522Rv1AR-FLAR-V7Inhibitorinhibitorinhibit

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