1. Autophagy Apoptosis
  2. Autophagy Apoptosis
  3. PFK-158

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria.

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PFK-158 Chemical Structure

PFK-158 Chemical Structure

CAS No. : 1462249-75-7

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
1 mg USD 38 In-stock
5 mg USD 80 In-stock
10 mg USD 130 In-stock
50 mg USD 350 In-stock
100 mg USD 550 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 6 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PFK-158 is a potent and selective PFKFB3 inhibitor with an IC50 value 137 nM. PFK-158 reduces glucose uptake, ATP production, lactate release, and induces apoptosis and autophagy in cancer cells. PFK-158 has broad anti-tumor activity. PFK-158 can also enhance Colistin's resistance to bacteria[1][2][3].

IC50 & Target

IC50 : 137 nM (PFKFB3)[1][3]

In Vitro

PFK-158 (10 µM ; 24 hours; OV2008 and C13 cells) combined with Carboplatin (CBPt; 77-453 μM) results in significant increase in apoptosis in C13 (45%) and OV2008 cells (24.6%)[1].
PFK-158 (0-10 µM ; 24 hours; C13 and HeyA8MDR cells) treatment results in a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels[1].
PFK-158 (10 μM; 24 hours) has synergistic anti-proliferative effects in vitro when combined with Cisplatin in C13 and HeyA8MDR cells compared to OV2008 and HeyA8, respectively[1].
PFK-158 (0‐10 μM; 24 h) treatment shows a dose-dependent downregulation of p62/SQSTM1 and upregulation of LC3BII, two markers of autophagy induction, in both C13 and HeyA8MDR cells. PFK-158 treatment also reduces the numbers of LDs[1].

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

Apoptosis Analysis[1]

Cell Line: OV2008 and C13 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Combined with Carboplatin (CBPt) treatment resulted in significant increase in apoptosis.

Western Blot Analysis[1]

Cell Line: C13 and HeyA8MDR cells
Concentration: 0 µM, 5 µM, 10 µM
Incubation Time: 24 hours
Result: Demonstrated a dose-dependent decrease in p-PFKFB3, p-cPLA2 and lipid droplet (LD) levels.
In Vivo

PFK-158 (15 mg/kg; intraperitoneal injection; once a week; for 4 weeks; female athymic nude mice) plus CBPt (51 mg/kg) treatment leads to significantly enhanced antitumor activity in a gynecologic cancer mouse model[1].

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

Animal Model: Female athymic nude mice (nu/nu) (5-6 weeks old) injected with HeyA8MDR cells[1]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; once a week; for 4 weeks
Result: A marked reduction of tumor growth was observed in the combination treatment.
Clinical Trial
Molecular Weight

328.29

Formula

C18H11F3N2O

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2

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 : ≥ 30 mg/mL (91.38 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0461 mL 15.2304 mL 30.4609 mL
5 mM 0.6092 mL 3.0461 mL 6.0922 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)

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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 mg/mL (6.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (6.09 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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:

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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

Purity: 98.88%

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 3.0461 mL 15.2304 mL 30.4609 mL 76.1522 mL
5 mM 0.6092 mL 3.0461 mL 6.0922 mL 15.2304 mL
10 mM 0.3046 mL 1.5230 mL 3.0461 mL 7.6152 mL
15 mM 0.2031 mL 1.0154 mL 2.0307 mL 5.0768 mL
20 mM 0.1523 mL 0.7615 mL 1.5230 mL 3.8076 mL
25 mM 0.1218 mL 0.6092 mL 1.2184 mL 3.0461 mL
30 mM 0.1015 mL 0.5077 mL 1.0154 mL 2.5384 mL
40 mM 0.0762 mL 0.3808 mL 0.7615 mL 1.9038 mL
50 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5230 mL
60 mM 0.0508 mL 0.2538 mL 0.5077 mL 1.2692 mL
80 mM 0.0381 mL 0.1904 mL 0.3808 mL 0.9519 mL
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PFK-158 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.

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Product Name:
PFK-158
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HY-12203
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