2. Autophagy
  3. Autophagy
  4. PFK-015

PFK-015 

Cat. No.: HY-12204 Purity: 98.29%
COA Handling Instructions

PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC).

For research use only. We do not sell to patients.

PFK-015 Chemical Structure

PFK-015 Chemical Structure

CAS No. : 4382-63-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 106 In-stock
50 mg USD 409 In-stock
100 mg USD 726 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE PFK-015

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC)[1][2].

IC50 & Target

IC50: 110 nM (recombinant PFKFB3); IC50: 20 nM (PFKFB3 activity in cancer cells)[2]
In Vitro

PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro[1].
PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity[1].
PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis[1].
PFK-015 potently inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM[2].
PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

PFK-015 impeds ESCC tumor growth in immunodeficient in vivo models[1].
PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression[1].
PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells[1].
PFK-015 enhances the efficacy of ESCC by enhancing CD8 + T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG[1].
PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

260.29

Appearance

Solid

Formula

C17H12N2O
CAS No.
SMILES

O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC=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 : 25.2 mg/mL (96.82 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8419 mL 19.2093 mL 38.4187 mL
5 mM 0.7684 mL 3.8419 mL 7.6837 mL
10 mM 0.3842 mL 1.9209 mL 3.8419 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2 mg/mL (7.68 mM); Clear solution

  • 2.

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

    Solubility: 2 mg/mL (7.68 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (7.68 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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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.

  • Molarity Calculator

  • Dilution Calculator

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

PFK-0154382-63-2PFK015PFK 015AutophagyPFKFB33POcancerslung cancerstomach cancercolon canceresophageal squamous cell carcinoma (ESCC)Inhibitorinhibitorinhibit

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