Fasentin

Research use only, not for human use.

Fasentin is a novel inhibitor of glucose uptake (GLUT) that sensitizes cancer cells to FAS-induced cell death, preferentially inhibits GLUT4 (IC50=68 uM) over GLUT1.

Fasentin is a novel inhibitor of glucose uptake (GLUT) that sensitizes cancer cells to FAS-induced cell death, preferentially inhibits GLUT4 (IC50=68 uM) over GLUT1; sensitizes cancer cells to the death ligands FAS and TNF apoptosis-inducing ligand, and induces G1 cell cycle arrest.

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.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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Fasentin

Membrane Transporter/Ion Channel

GLUT

GLUT

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392721-37-8

279.643

C11H9ClF3NO2

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (357.60 mM)

CC(CC(NC1=CC=C(Cl)C(C(F)(F)F)=C1)=O)=O

N-[4-Chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide

(-20℃)

With Ice Pack

≥ 2 years