AKB-6899

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

AKB-6899 是脯氨酰羟化酶结构域 3 (PHD3) 的抑制剂，可增加经 GM-CSF 处理的巨噬细胞产生可溶性 VEGF 受体 (sVEGFR-1)。

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

Western Blot Analysis Cell Line:Murine bone marrow-derived macrophages Concentration:10 μM Incubation Time:24 hours Result:Observed an increase in HIF-2α protein in cells.

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.

AKB 6899 | AKB6899

Angiogenesis

VEGFR

Human H3 receptor

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1007377-55-0

290.25

C14H11FN2O4

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (344.53 mM)

OC(=O)CNC(=O)c1ncc(cc1O)-c1cccc(F)c1

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(-20℃)

With Ice Pack

≥ 2 years