AKB-6899 是脯氨酰羟化酶结构域 3 (PHD3) 的抑制剂，可增加 GM-CSF 处理的巨噬细胞产生的 VEGF 受体的可溶形式 (sVEGFR-1)。 AKB-6899 能稳定 HIF-2α，从而诱导肿瘤相关巨噬细胞产生 sVEGFR-1 并减少肿瘤生长。

AKB-6899 is an inhibitor of prolyl hydroxylase domain 3 (PHD3) and increases the soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages. AKB-6899 leads to stabilization of HIF-2α which induces sVEGFR-1 production from tumor-associated macrophages and decreases tumor growth.

In murine bone marrow-derived macrophages, AKB-6899 (10 μM; 24 hours) increases the levels of HIF-2α protein, with no corresponding increase in HIF-1α. AKB-6899 shows no effect on HIF-1α accumulation or VEGF production[1].

In C57BL/6 mice injected with B16F10 murine melanoma cells, AKB-6899 (17.5 mg/kg; i.p.) significantly reduces tumor growth[1].

1007377-55-0

C14H11FN2O4

290.25

AKB6899

DMSO:95 mg/mL (327.30 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years