| Identification | Back Directory | [Name]
PFK-015 | [CAS]
4382-63-2 | [Synonyms]
CS-1317
PFK-015
PFK15 (PFK-015)
PFK015;PFK15;PFK 15;PFK-15
1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
1-(Pyridin-4-yl)-3-(quinolin-2-yl)prop-2-en-1-one
2-Propen-1-one, 1-(4-pyridinyl)-3-(2-quinolinyl)-
1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one PFK15 | [Molecular Formula]
C17H12N2O | [MDL Number]
MFCD28099813 | [MOL File]
4382-63-2.mol | [Molecular Weight]
260.29 |
| Chemical Properties | Back Directory | [Boiling point ]
464.4±45.0 °C(Predicted) | [density ]
1.237±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
3.11±0.61(Predicted) | [color ]
white to beige | [Stability:]
Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. | [InChI]
1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+ | [InChIKey]
UJJUKZPBUMCSJZ-BQYQJAHWSA-N | [SMILES]
n1ccc(cc1)C(=O)\C=C\c2nc3c(cc2)cccc3 |
| Hazard Information | Back Directory | [Description]
PFK15 (4382-63-2) is an inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3).? PFKFB3 is constitutively expressed by neoplastic cells and is required for the high glycolytic rate (Warburg Effect) of these cells. PFK15 inhibits PFKFB3 (IC50?= 207 nM) without inhibiting 96 other kinases.1?PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growth?in vitro?and?in vivo.?PFK15 has been shown to inhibit tumor growth in various cancer models.2,3 | [Uses]
PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells. | [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]. | [storage]
Store at -20°C | [References]
1) Clem?et al.?(2013),?Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol. Cancer Ther.?12?1461
2) Zhu?et al. (2016),?PFK15,a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer; PLoS One?11?e0163768
3) Li?et al. (2017),?Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma; J. Exp. Clin. Cancer Res.?36?7 |
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| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|