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| Company | Aladdin Scientific Corporation | Aladdin Scientific Corporation | Aladdin Scientific Corporation | Aladdin Scientific Corporation | Aladdin Scientific Corporation |
| Item | PFK15 | 1H-Pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione | H2L5186303 | rel-(1S,2S,5R)-6-oxo-3-azabicyclo[3.2.0]heptane-2-carboxylic acid;2,2,2-trifluoroacetic acid | Sebacic acid |
| Catalog Number | P170364 | H194444 | H287312 | R638105 | S420619 |
| Price | Supplier Page | Supplier Page | Supplier Page | Supplier Page | Supplier Page |
| Description | PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM. IC50 value: 110 nM (recombinant PFKFB3)[1] Target: PFKFB3 PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents,PFK-015 is an effective inhibitor of PFKFB3 with IC50 of 110 nM (recombinant PFKFB3) and inhibits PFKFB3 activity in cancer cells with IC50 of 20 nM. IC50 value: 110 nM (recombinant PFKFB3)[1] Target: PFKFB3 PFK-015 possesses compelling in vitro properties, has satisfactory PK properties in rodents, and suppresses tumor glucose metabolism and growth in an aggressive mouse model of non-small cell lung cancer. PFK-015 is not a Pgp substrate as determined by transport and cell permeability assays in Caco-2 and MDCK-MDR1 (Papp A-B / B-A results 1.8 / 4 and 5 / 5 10–6 cm/s). PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines. PFK-015 suppresses glucose uptake in cancer cells. Rodent PK studies following IV dosing at 5 mg/kg resulted in a profile with a satisfactory half-life (5.1 hours), exposure (AUCinf 1804 ng.h/ml), tissue distribution (Vd 20.5 L/kg) and reasonable clearance (46.2 mL/min/kg). Also, pre-clinical efficacy studies of C57Bl/6 mice bearing Lewis Lung Carcinoma (LLC) xenografts demonstrated 80% tumor growth inhibition relative to vehicle control. Finally, micro-PET studies performed on mice bearing LLC tumors showed a significant inhibition of tumor 2-[18F]-fluoro-2-deoxy-glucose uptake. These results support further development of PFK-015 as a novel anti-cancer agent... Read More | Inquire | Inquire | Inquire | Inquire |
| Quantity | 100mg, 5mg, 25mg | 250mg, 5g, 1g | 100mg, 5mg, 50mg, 10mg, 25mg | 1g | 1ml |
| Type | Chelating Agents & Ligands | Organic Compound | Chelating Agents & Ligands | Aromatic Compound | Organic Compound |
| Purity / Grade | ≥98%(HPLC), Moligand™, ≥98%(HPLC) | ≥97% | ≥98%(HPLC), Moligand™, ≥98%(HPLC) | ≥97% | 10mM in DMSO |
| SMILES | C1=CC=C2C(=C1)C=CC(=N2)/C=C/C(=O)C3=CC=NC=C3 | C1=CNC2=C1NC(=O)NC2=O | C1=CC(=CC(=C1)OC2=CC=C(C=C2)NC(=O)/C=C\C(=O)O)OC3=CC=C(C=C3)NC(=O)/C=C\C(=O)O | Inquire | C(CCCCC(=O)O)CCCC(=O)O |
| Molecular Formula | C17H12N2O | C6H5N3O2 | C₂₆H₂₀N₂O₈ | Inquire | C10H18O4 |
| Applications | Inquire | Inquire | Inquire | Inquire | Inquire |
| Get Quote | Supplier Page | Supplier Page | Supplier Page | Supplier Page | Supplier Page |