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Formula | C17 H12 N2 O |
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Molecular Weight | 260.29 | CAS No. | 4382-63-2 | ||||||||
Solubility (25°C)* | In vitro | DMSO | 52 mg/mL (199.77 mM) | ||||||||
Ethanol | 20 mg/mL (76.83 mM) | ||||||||||
Water | Insoluble | ||||||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | PFK15 (PFK-015) is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM. | ||
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Targets |
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In vitro | PFK15 produces potent growth inhibition in a series of cancer cells. In Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells, PFK15 also reduces F26BP, glucose uptake, and intracellular ATP level. [1] | ||
In vivo | In vivo, PFK15 has adequate pharmacokinetic properties. PFK15 (25 mg/kg i.p.) suppresses the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three human xenograft models of cancer in athymic mice, PFK15 also yields antitumor effects that are comparable to approved chemotherapeutic agents. [1] |
Kinase Assay: |
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Cell Assay: |
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Animal Study: |
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, , J Exp Clin Cancer Res, 2017, 36(1):7
Data from [Data independently produced by , , Br J Pharmacol, 2017, 174(9):893-908]
Data from [Data independently produced by , , PLoS One, 2016, 11(9):e0163768]
Identification of PFKFB3 as a key factor in the development of colorectal cancer and immunotherapy resistance [ Clin Exp Med, 2024, 24(1):219] | PubMed: 39261380 |
Multi-omics and immunogenomics analysis revealed PFKFB3 as a targetable hallmark and mediates sunitinib resistance in papillary renal cell carcinoma: in silico study with laboratory verification [ Eur J Med Res, 2024, 29(1):236] | PubMed: 38622715 |
Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] | PubMed: 37689702 |
Human blood vessel organoids reveal a critical role for CTGF in maintaining microvascular integrity [ Nat Commun, 2023, 14(1):5552] | PubMed: 37689702 |
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] | PubMed: 37649137 |
Arginine methylation of PPP1CA by CARM1 regulates glucose metabolism and affects osteogenic differentiation and osteoclastic differentiation [ Clin Transl Med, 2023, 13(9):e1369] | PubMed: 37649137 |
PFKFB3-mediated Pro-glycolytic Shift in Hepatocellular Carcinoma Proliferation [ Cell Mol Gastroenterol Hepatol, 2023, 15(1):61-75] | PubMed: 36162723 |
Long noncoding RNA LINC00930 promotes PFKFB3-mediated tumor glycolysis and cell proliferation in nasopharyngeal carcinoma [ J Exp Clin Cancer Res, 2022, 41(1):77] | PubMed: 35209949 |
CYLD deficiency enhances metabolic reprogramming and tumor progression in nasopharyngeal carcinoma via PFKFB3 [ Cancer Lett, 2022, S0304-3835(22)00055-6] | PubMed: 35131382 |
Metabolic reprogramming by dual-targeting biomimetic nanoparticles for enhanced tumor chemo-immunotherapy [ Acta Biomater, 2022, 148:181-193] | PubMed: 35649505 |
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.