N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
![N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide,392721-37-8,结构式](https://www.chemicalbook.com/CAS/20200331/GIF/392721-37-8.gif)
- CAS号:392721-37-8
- 英文名:N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
- 中文名:N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
- CBNumber:CB21845028
- 分子式:C11H9ClF3NO2
- 分子量:279.64
- MOL File:392721-37-8.mol
- 沸点 :394.2±42.0 °C(Predicted)
- 密度 :1.411±0.06 g/cm3(Predicted)
- 储存条件 :room temp
- 溶解度 :DMSO: >10mg/mL
- 形态 :powder
- 酸度系数(pKa) :10.76±0.46(Predicted)
- 颜色 :white to off-white
- 稳定性 :Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide性质、用途与生产工艺
- 生物活性 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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靶点
GLUT4
68 μM (IC 50 )
GLUT1
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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 (IC 50 =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 [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.
- 更新日期：2024/11/08
- 产品编号：HY-101849
- 产品名称：N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide Fasentin
- CAS编号：392721-37-8
- 包装：5mg
- 价格：700元
- 更新日期：2024/11/08
- 产品编号：HY-101849
- 产品名称：N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide Fasentin
- CAS编号：392721-37-8
- 包装：10mM * 1mLin DMSO
- 价格：770元
- 公司名称：Carbosynth
- 联系电话：--
- 电子邮件：sales@carbosynth.com
- 国家：英国
- 产品数：6005
- 优势度：58
- 公司名称：TOCRIS-US
- 联系电话：--
- 电子邮件：customerservice@tocris.co.uk
- 国家：英国
- 产品数：5726
- 优势度：77
