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。
| 生物活性 |
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. |
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| 体外研究 |
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. Western Blot Analysis
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| 体内研究 |
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.
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| 分子式 |
C14H11FN2O4
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| 分子量 |
290.25
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| CAS号 |
1007377-55-0
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| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
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| 储存方式 |
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纯度： 98%
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