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PFK-158 

Cat. No.: HY-12203 Purity: 98.85%
Handling Instructions

PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies.

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

PFK-158 Chemical Structure

PFK-158 Chemical Structure

CAS No. : 1462249-75-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 290 In-stock
Estimated Time of Arrival: December 31
100 mg USD 450 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

PFK-158 is a potent and selective inhibitor of PFKFB3 that is currently being investigated in a phase I study in patients with advanced solid malignancies. Target: PFKFB3 in vitro: PFK-158 is the first 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) inhibitor to undergo clinical trial testing in cancer patients. PFK-158, a small molecule therapeutic candidate that inactivates a novel cancer metabolism target never before examined in human clinical trials. PFK-158 is not only a first-in-class cancer drug but also the first to target glucose metabolism by inhibiting PFKFB3. PFK-158 is a nanomolar inhibitor of recombinant PFKFB3. PFK-158 inhibits PFKFB3 activity and glycolysis in cancer cells. in vivo: PFK158 is well tolerated in rats and dogs resulting in an acceptable pre-clinical therapeutic index. PFK158 is very effective in multiple preclinical mouse models of human-derived tumors and syngeneic murine models. IND-enabling safety and toxicity studies demonstrated that PFK158 is well tolerated in rats and dogs and supported the initiation of a phase I trial that is now underway.

Clinical Trial
Molecular Weight

328.29

Formula

C₁₈H₁₁F₃N₂O

CAS No.

1462249-75-7

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)

*"≥" 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
10 mM 0.3046 mL 1.5230 mL 3.0461 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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PFK-158
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HY-12203
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