AKB-6899|cas:1007377-55-0|西域试剂

AKB-6899,99.58%

产品编号：Bellancom-113649| CAS NO：1007377-55-0| 分子式：C₁₄H₁₁FN₂O₄| 分子量：290.25

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货号	价格	库存与货期
Bellancom-113649	￥2200.00	杭州北京（现货）
Bellancom-113649	￥3500.00	杭州北京（现货）
Bellancom-113649	￥7400.00	杭州北京（现货）
Bellancom-113649	￥12000.00	杭州北京（现货）

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AKB-6899

产品介绍

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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.

西域 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.

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.

西域 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.

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.

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (344.53 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.4453 mL	17.2265 mL	34.4531 mL
5 mM	0.6891 mL	3.4453 mL	6.8906 mL
10 mM	0.3445 mL	1.7227 mL	3.4453 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。