PFK-158
Modify Date: 2025-08-25 12:25:01
PFK-158 structure
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Common Name | PFK-158 | ||
|---|---|---|---|---|
| CAS Number | 1462249-75-7 | Molecular Weight | 328.288 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | 466.3±45.0 °C at 760 mmHg | |
| Molecular Formula | C18H11F3N2O | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 235.8±28.7 °C | |
Use of PFK-158PFK-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. |
| Name | PFK-158 |
|---|---|
| Synonym | More Synonyms |
| 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: 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. |
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| Related Catalog | |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Boiling Point | 466.3±45.0 °C at 760 mmHg |
| Molecular Formula | C18H11F3N2O |
| Molecular Weight | 328.288 |
| Flash Point | 235.8±28.7 °C |
| Exact Mass | 328.082336 |
| LogP | 3.55 |
| Vapour Pressure | 0.0±1.2 mmHg at 25°C |
| Index of Refraction | 1.624 |
| InChIKey | IAJOMYABKVAZCN-AATRIKPKSA-N |
| SMILES | O=C(C=Cc1ccc2ccc(C(F)(F)F)cc2n1)c1ccncc1 |
| Storage condition | 2-8℃ |
| 2-Propen-1-one, 1-(4-pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-, (2E)- |
| (2E)-1-(4-Pyridinyl)-3-[7-(trifluoromethyl)-2-quinolinyl]-2-propen-1-one |