Fasentin|392721-37-8|-陌孚医药/Medlife

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Fasentin

目录号: PL01300 纯度: ≥98%

CAS No. :392721-37-8

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中文名称	Fasentin
中文别名	N-[4-Chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
英文名称	Fasentin
英文别名	N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide;Glucose Transporter Inhibitor;ST51005182;N-(4-Chloro-3-(trifluoromethyl)phenyl)-3-oxobutanamide;Fasentin;ZINC00449608;AC1LGZUC;CBMicro_009435;AC1Q1K2J;CTK7G4986;Glucose Transporter Inhibitor; ST51005182; N-(4-Chloro-3-(trifluoromethyl)phenyl)-3-oxobutanamide; Fasentin; ZINC00449608; AC1LGZUC; CBMicro_009435; AC1Q1K2J; CTK7G4986;
Cas No.	392721-37-8
分子式	C₁₁H₉ClF₃NO₂
分子量	279.64
包装储存	Pure form -20°C 3 years；4°C 2 years

产品详情	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, inhibits GLUT-1/GLUT-4 transporters. Fasentin preferentially inhibits GLUT4 (IC 50 =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.
性状	Oil
IC50 & Target[1][2]	GLUT4 68 μM (IC50) GLUT1
体外研究(In Vitro)	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
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
参考文献	[1]. Ma Carmen Oca?a, et al. Fasentin diminishes endothelial cell proliferation, differentiation and invasion in a glucose metabolism-independent manner. Sci Rep. 2020 Apr 9;10(1):6132. [2]. Tabitha E Wood, et al. A novel inhibitor of glucose uptake sensitizes cells to FAS-induced cell death. Mol Cancer Ther. 2008 Nov;7(11):3546-55.

溶解度数据	In Vitro: DMSO : 100 mg/mL (357.60 mM; Need ultrasonic)配制储备液

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