AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects. In Vitro AKB-6899 (10 μM; 24 hours) increases the leves of HIF-2α protein, with no corresponding increase in HIF-1α. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, with no effect on HIF-1α accumulation or VEGF production. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Murine bone marrow-derived macrophages Concentration: 10 μM Incubation Time: 24 hours Result: Observed an increase in HIF-2α protein in cells. In Vivo AKB-6899 (17.5 mg/kg; i.p.; 3 times per week; for 16 days) treatment significantly reduces tumor growth in a murine melanoma model . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8-week-old C57BL/6 mice injected with B16F10 murine melanoma cells Dosage: 17.5 mg/kg Administration: i.p.; 3 times per week; for 16 days Result: Significantly reduced tumor growth. Form:Solid
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AKB-6899
CAS number：1007377-55-0 molecular formula：C14H11FN2O4
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| Chinese alias | - | ||
| English alias | SCHEMBL3484399 | UNII-ZIA31378BO | 2-[[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]amino]acetic acid | Q27295569 | {[5-(3-fluoro-phenyl)-3-hydroxypyridine-2-carbonyl]-amino}acetic acid | {[5-(3-fluorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic a | ||
| CAS number | 1007377-55-0 | molecular formula | C14H11FN2O4 |
| molecular weight | 290.25 g/mol | Exact mass | ≥99% |
| PSA | 99.500 Ų | logp | 2.000 |
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