AKB-6899 是一种脯氨酰羟化酶域 3 (PHD3) 抑制剂，是一种选择性 HIF-2α 稳定剂。AKB-6899 还增加了 GM-CSF 处理的巨噬细胞产生的 sVEGFR-1，并具有抗肿瘤和抗血管生成作用。
货号:ajcx33404
CAS:1007377-55-0
分子式:C14H11FN2O4
分子量：290.25
溶解度:N/A
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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[1].

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[1].

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[1].

[1]. Julie M Roda, et al. Stabilization of HIF-2α induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth in a murine melanoma model. J Immunol. 2012 Sep 15;189(6):3168-77.