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Fasentin

Cat No.:V19961 Purity: ≥98%
Fasentin is a potent glucose uptake inhibitor that can suppress the GLUT-1/GLUT-4 transporter.
Fasentin
Fasentin Chemical Structure CAS No.: 392721-37-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Fasentin is a potent glucose uptake inhibitor that can suppress the GLUT-1/GLUT-4 transporter. Fasentin preferentially inhibits GLUT4 (IC50=68 μM). Fasentin is a death receptor stimulation (FAS) sensitizer that sensitizes cells to FAS-induced cell death. Fasentin is also a sensitizer for the apoptotic ligand-induced tumor necrosis factor (TNF). Fasentin blocks glucose uptake in cancer/tumor cell lines and has anti-angiogenic activity.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Fasentin (0.1-1000 μM; 72 hours) inhibits the growth of endothelial cells, tumors, and fibroblasts without causing cell death [1]. Fasentin (25-100 μM; 16-24 hours) induces cell cycle arrest in the G0/G1 phase and decreases the number of S-phase cells in a dose-dependent manner [1]. Fasentin (50 μM; 16 hours) modifies the expression of genes linked to glucose deprivation, such as AspSyn and PCK-2[2]. Fasentin (15, 30, 80 μM; 1 hour pretreatment) induces glucose deprivation and partially blocks glucose uptake in PPC-1, DU145, and U937 cells [2]. Fasentin (100 μM; 16 hours) has no effect on endothelial cell migration [1]. Fasentin (25–100 μM; 16 hours) decreased phospho-ERK levels in HMEC, indicating partial inhibition of the ERK signaling pathway, though the effect was not statistically significant.
Cell Assay
Cell viability assay [1]
Cell Types: three endothelial cell ECs (HMEC, human microvascular endothelial cells; HUVEC, human umbilical vein endothelial cells; and BAEC, bovine aortic endothelial cells), three human tumor cell lines (MDA-MB - 231 and MCF7 breast cancer cells, HeLa cervical adenocarcinoma cells) and human gingival fibroblasts (HGF)
Tested Concentrations: 0.1, 1, 10, 100, 1000 μM
Incubation Duration: 72 hrs (hours)
Experimental Results: Inhibition of endothelial cells, tumors and fibroblasts cell growth (IC50 =26.3-111.2 μM) and does not induce cell death.

Cell cycle analysis [1]
Cell Types: HMEC
Tested Concentrations: 25, 50, 100 μM
Incubation Duration: 16, 24 hrs (hours)
Experimental Results: Induced cell cycle arrest in G0/G1 phase and diminished the number of S phase cells in a dose-dependent manner. There was no increase in the subG1 population.

RT-PCR[2]
Cell Types: PPC-1 cells[2]
Tested Concentrations: 50 μM
Incubation Duration: 16 hrs (hours)
Experimental Results: Altered expression of genes associated with glucose deprivation such as AspSyn and PCK-2 not FLIP mRNA expression.
References

[1]. Fasentin diminishes endothelial cell proliferation, differentiation and invasion in a glucose metabolism-independent manner. Sci Rep. 2020 Apr 9;10(1):6132.

[2]. A novel inhibitor of glucose uptake sensitizes cells to FAS-induced cell death. Mol Cancer Ther. 2008 Nov;7(11):3546-55.

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

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H9CLF3NO2
Molecular Weight
279.642872571945
Exact Mass
279.027
CAS #
392721-37-8
PubChem CID
879520
Appearance
Light yellow to brown ointment
Melting Point
141.7 °C
LogP
3.925
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
3
Heavy Atom Count
18
Complexity
333
Defined Atom Stereocenter Count
0
SMILES
CC(CC(NC1=CC(C(F)(F)F)=C(Cl)C=C1)=O)=O
InChi Key
GNYIJZMBLZXJEJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H9ClF3NO2/c1-6(17)4-10(18)16-7-2-3-9(12)8(5-7)11(13,14)15/h2-3,5H,4H2,1H3,(H,16,18)
Chemical Name
N-[4-chloro-3-(trifluoromethyl)phenyl]-3-oxobutanamide
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~357.60 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.94 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: 2.5 mg/mL (8.94 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (8.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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