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PFK-158 Catalog No.GC19293

A PFKFB3 inhibitor

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 1462249-75-7 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC(C(F)(F)F)=CC=C3C=C2
Formula C18H11F3N2O M.Wt 328.29
Solubility DMSO : ≥ 30 mg/mL (91.38 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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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: PFKFB3in 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.

[1]. Rebecca Redman, et al. Abstract CT206: PFK-158, first-in-man and first-in-class inhibitor of PFKFB3/ glycolysis: A phase I, dose escalation, multi-center study in patients with advanced solid malignancies. Cancer Res August 1, 2015 75; CT206. doi: 10.1158
[2]. Sucheta Telang, et al. Discovery of a PFKFB3 inhibitor for phase I trial testing that synergizes with the B-Raf inhibitor vemurafenib. Cancer Metab. 2014; 2(Suppl 1): P14.