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| Cas No.: | 1462249-75-7 |
| Chemical Name: | (E)-1-(pyridin-4-yl)-3-(7-(trifluoromethyl)quinolin-2-yl)prop-2-en-1-one |
| Synonyms: | PFK-158,PFK 158 |
| 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 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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. |
| 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. |