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。
| 生物活性 | Fasentin, a potent glucose uptake inhibitor, inhibitsGLUT-1/GLUT-4transporters. Fasentin preferentially inhibitsGLUT4(IC50=68 μM) overGLUT1. Fasentin is adeath receptorstimuli (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 incancercell lines and has anti-angiogenic activity[1][2][3]. |
| IC50& Target[1][3] | |
体外研究
(In Vitro) | Fasentin (0.1-1000 μM; 72 hours) inhibits endothelial, tumour and fibroblast cell growth without inducing cell death[1].
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[1].
Fasentin (50 μM; 16 hours) alters expression of genes associated with glucose deprivation such as AspSyn and PCK-2[2].
Fasentin (15, 30, 80 μM; pretreatment 1 hour) induces glucose deprivation, partially blocks glucose uptake in PPC-1, DU145, and U937 cells[2].
Fasentin (100 μM; 16 hours) does not affect the migratory capability of endothelial cells[1].
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[1].
Fasentin interacts with a unique site in the intracellular channel of GLUT1[3].
Cell Viability Assay[1] | 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[1] | 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[2] | Cell Line: | PPC-1 cells[2] | | 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(357.60 mM;Need ultrasonic) 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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-CDin 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 μL20% 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。 *以上所有助溶剂都可在本网站选购。
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