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  • DC Chemicals Limited
  • China
  • Product Name: Fasentin
  • Price: $500.0/100mg $900.0/250mg $1750.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

392721-37-8

392721-37-8 structure
392721-37-8 structure
  • Name: Fasentin
  • Chemical Name: N-[4-Chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
  • CAS Number: 392721-37-8
  • Molecular Formula: C11H9ClF3NO2
  • Molecular Weight: 279.64300
  • Catalog: Research Areas Cardiovascular Disease
  • Create Date: 2017-12-14 21:42:40
  • Modify Date: 2024-01-29 06:53:36
  • 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[1][2][3].

Name N-[4-Chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
Synonyms N-(4-Chloro-3-(trifluoromethyl)phenyl)-3-oxobutanamide
Glucose Transporter Inhibitor
Fasentin
Description 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[1][2][3].
Related Catalog
Target

GLUT4:68 μM (IC50)

GLUT1

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.
References

[1]. Mª Carmen Ocaña, 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.

[3]. Qin Wu, et al. GLUT1 inhibition blocks growth of RB1-positive triple negative breast cancer. Nat Commun. 2020 Aug 21;11(1):4205.

Melting Point 141.7 °C
Molecular Formula C11H9ClF3NO2
Molecular Weight 279.64300
Exact Mass 279.02700
PSA 49.66000
LogP 3.92590
Storage condition 2-8°C
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Hazard Codes Xn
RIDADR NONH for all modes of transport
HS Code 2924299090
HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%