Fasentin - CAS:392721-37-8

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Fasentin

目录号 : KM4243 CAS No. : 392721-37-8 纯度 : ≥98%

Data Sheet 产品使用指南

Fasentin 是有效的葡萄糖摄取抑制剂，可抑制 GLUT-1/GLUT-4 转运蛋白。Fasentin 优先抑制 GLUT4 (IC₅₀=68 μM)。Fasentin 是死亡受体刺激 (FAS) 敏化剂，可敏化细胞对 FAS 诱导的细胞死亡。Fasentin 也是诱导肿瘤坏死因子 (TNF) 凋亡配体的敏化剂。Fasentin 阻断癌细胞系中的葡萄糖摄取，并具有抗血管生成活性。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

Fasentin, a potent glucose uptake inhibitor, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC₅₀=68 μM) over GLUT1. Fasentin is a death receptor stimuli (FAS) sensitizer and sensitizes cells to FAS-induced cell death. Fasentin is also a tumor necrosis factor (TNF) apoptosis-inducing ligand sensitizer. Fasentin blocks glucose uptake in cancer cell lines and has anti-angiogenic activity.

体外研究

Fasentin (0.1-1000 μM; 72 hours) inhibits endothelial, tumour and fibroblast cell growth without inducing cell death.
Fasentin (25-100 μM; 16-24 hours) induces a cell cycle arrest in G0/G1 phase and reduces the cell number in S phase in a dose-dependent manner.
Fasentin (50 μM; 16 hours) alters expression of genes associated with glucose deprivation such as AspSyn and PCK-2.
Fasentin (15, 30, 80 μM; pretreatment 1 hour) induces glucose deprivation, partially blocks glucose uptake in PPC-1, DU145, and U937 cells.
Fasentin (100 μM; 16 hours) does not affect the migratory capability of endothelial cells.
Fasentin (25-100 μM; 16 hours) lowers levels of phospho-ERK in HMECs, indicating a partial inhibition on the ERK signalling pathway, even though the effect is not statistically significant. Fasentin does not inhibit the tyrosine kinase activity of VEGFR2.
Fasentin interacts with a unique site in the intracellular channel of GLUT1.

Cell Viability Assay

Cell Line:	Three types of endothelial cells ECs (HMEC, human microvascular endothelial cells; HUVEC, human umbilical vein endothelial cells; and BAEC, bovine aortic endothelial cells), three human tumour cell lines (MDA-MB-231 and MCF7 breast carcinoma cells, and HeLa cervix adenocarcinoma cells), and human gingival fibroblasts (HGF)
Concentration:	0.1, 1, 10, 100, 1000 μM
Incubation Time:	72 hours
Result:	Inhibited endothelial, tumour and fibroblast cell growth (IC₅₀=26.3-111.2 μM) without inducing cell death.

Cell Cycle Analysis

Cell Line:	HMECs
Concentration:	25, 50, 100 μM
Incubation Time:	16, 24 hours
Result:	Induced a cell cycle arrest in G0/G1 phase and reduced the cell number in S phase in a dose-dependent manner. Did not increase the subG1 population.

RT-PCR

Cell Line:	PPC-1 cells
Concentration:	50 μM
Incubation Time:	16 hours
Result:	Altered expression of genes associated with glucose deprivation such as AspSyn and PCK-2 not FLIP mRNA expression.

分子式

C₁₁H₉ClF₃NO₂

分子量

279.64

CAS号

392721-37-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL (357.60 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5760 mL	17.8801 mL	35.7603 mL
5 mM	0.7152 mL	3.5760 mL	7.1521 mL
10 mM	0.3576 mL	1.7880 mL	3.5760 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 (8.94 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.94 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。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: 2.5 mg/mL (8.94 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (8.94 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (8.94 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (8.94 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。