AKB-6899 (C09-1102-894)

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 VitroAKB-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 VivoAKB-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. Specification: 0.99 Molecular Formula: C14H11FN2O4 Molecular Weight: 290.25 PubChem CID: 49848485 Isomeric SMILES: C1=CC(=CC(=C1)F)C2=CC(=C(N=C2)C(=O)NCC(=O)O)O