GN44028|cas:1421448-26-1|西域试剂

GN44028,99.37%

产品编号：Bellancom-110266| CAS NO：1421448-26-1| 分子式：C₁₈H₁₅N₃O₂| 分子量：305.33

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-110266		￥2900.00	杭州北京（现货）

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GN44028

产品介绍

GN44028 是一种有效的、具有口服活性的缺氧诱导因子-1α (HIF-1α) 抑制剂，其 IC₅₀ 值为 14 nM。GN44028 能抑制低氧诱导的 HIF-1α 的转录活性，但不抑制 HIF-1α mRNA 的表达，HIF-1α 蛋白的累积或 HIF-1α/HIF-1β 的异缘二聚化。GN44028 可用于癌症的研究。

生物活性

GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC₅₀ of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers.

体外研究

GN44028 (compound 2I, 0-30 µM approximately) has anti-proliferative activities against HCT116, HepG2 and HeLa cells.
GN44028 (0.001-1 μM, 4 h) inhibits the hypoxia-induced VEGF mRNA expression in HeLa cells.
GN44028 (20 nM, 10 days) abrogates the TGF‐β‐induced colony formation in HCT116 cells.

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

RT-PCR

Cell Line:	HeLa cells
Concentration:	0.001, 0.01, 0.1, 1µM
Incubation Time:	4 h
Result:	Inhibited the hypoxia-induced HIF-1 transcriptional activity without affecting HIF-1α/HIF-1β heterodimerization.

体内研究
(In Vivo)

GN44028 (10 mg/kg, oral gavage) extends the survival rate of animals in mice bearing a mixed orthotopic tumor with PN12 and ME23 cells.
GN44028 (5 mg/kg, tail vein injection, twice a week) suppresses tumor growth in a subcutaneous colorectal cancer model.

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

Animal Model:	Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells
Dosage:	10 mg/kg
Administration:	Oral gavage
Result:	Reduced both proneural and mesenchymal markers.

Animal Model:	Subcutaneous colorectal cancer model (HCT116)
Dosage:	5 mg/kg
Administration:	Tail vein injection, twice a week
Result:	Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.

体内研究

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

Animal Model:	Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells
Dosage:	10 mg/kg
Administration:	Oral gavage
Result:	Reduced both proneural and mesenchymal markers.

Animal Model:	Subcutaneous colorectal cancer model (HCT116)
Dosage:	5 mg/kg
Administration:	Tail vein injection, twice a week
Result:	Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.

体内研究

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

Animal Model:	Mice bearing a mixed orthotopic tumor with PN12 and ME23 cells
Dosage:	10 mg/kg
Administration:	Oral gavage
Result:	Reduced both proneural and mesenchymal markers.

Animal Model:	Subcutaneous colorectal cancer model (HCT116)
Dosage:	5 mg/kg
Administration:	Tail vein injection, twice a week
Result:	Reduced pulmonary nodules in tumor-bearing mice, and enhanced the outcome of chemotherapy.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (163.76 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.2751 mL	16.3757 mL	32.7515 mL
5 mM	0.6550 mL	3.2751 mL	6.5503 mL
10 mM	0.3275 mL	1.6376 mL	3.2751 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 (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 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 (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 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 (8.19 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.19 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。