STF-31

Alias: STF31; STF-31; STF 31
Cat No.:V1876 Purity: ≥98%
STF-31 is anovel potent and selective glucose transporter (GLUT1) inhibitor with IC50 of 1 μM.
STF-31 Chemical Structure CAS No.: 724741-75-7
Product category: Glutaminase
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

STF-31 is a novel potent and selective glucose transporter (GLUT1) inhibitor with IC50 of 1 μM. By targeting glucose uptake through GLUT1 specifically and taking advantage of the distinct reliance of these cells on GLUT1 for survival, STF31 kills RCCs in a selective manner. By directly binding to GLUT1 and preventing glucose uptake in vivo, STF31 treatment prevents the growth of RCCs without harming healthy tissue. STF-31 selectively removes hPSCs from mixed cultures and is toxic to hPSCs.

Biological Activity I Assay Protocols (From Reference)
Targets
GLUT1 (IC50 = 1 μM)
ln Vitro
STF-31 specifically targets glucose uptake through GLUT1, which kills RCCs with selectivity. STF-31 reduces glucose transport, which lowers glycolysis, and dramatically inhibits lactate production and extracellular acidification in VHL-deficient cells by approximately 60%. (Source: ) By preventing NAMPT's enzymatic activity, STF-31 exhibits cytotoxicity in cells that express NAPRT1.[2] STF-31 selectively eliminates hPSCs from mixed cultures and is toxic to hPSCs.[3]
ln Vivo
More soluble STF-31 analogue (11.6 mg/kg, i.p.) significantly inhibits tumor growth in mice bearing RCC xenografts deficient in VHL. [1]
Cell Assay
Five thousand cells are plated in 96-well plates for XTT assays. The following day, the drug or vehicle (DMSO) is added by serial dilution. After aspirating the media four days later, the plates are incubated at 37°C for one to two hours. The XTT solution (0.3 mg/ml of XTT, 2.65 μg/ml N-methyl dibenxopyrazine methyl sulfate in phenol red-free media) is then added. The absorbance at 450 nm is used to quantify the metabolism of XTT. One method for calculating IC50s is linear interpolation. Every experiment is carried out in duplicate or triplicate, and all conditions are measured in triplicate.
Animal Protocol
Mice with VHL-deficient RCC xenografts
11.6 mg/kg
i.p.
References

[1]. Design, Synthesis, and Antiviral Activity of 2'-Deoxy-2'-fluoro-2'-C-methyl-cytidine, a Potent Inhibitor of Hepatitis C Virus Replication. J Med Chem. 2005 Aug 25;48(17):5504-8.

[2]. ACS Chem Biol . 2014 Oct 17;9(10):2247-54.

[3]. Stem Cell Reports . 2014 Jun 6;3(1):185-203.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H25N3O3S
Molecular Weight
423.53
Exact Mass
423.16
Elemental Analysis
C, 65.23; H, 5.95; N, 9.92; O, 11.33; S, 7.57
CAS #
724741-75-7
Appearance
Solid powder
SMILES
CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NCC2=CC=C(C=C2)C(=O)NC3=CN=CC=C3
InChi Key
NGQPRVWTFNBUHA-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H25N3O3S/c1-23(2,3)19-10-12-21(13-11-19)30(28,29)25-15-17-6-8-18(9-7-17)22(27)26-20-5-4-14-24-16-20/h4-14,16,25H,15H2,1-3H3,(H,26,27)
Chemical Name
4-[[(4-tert-butylphenyl)sulfonylamino]methyl]-N-pyridin-3-ylbenzamide
Synonyms
STF31; STF-31; STF 31
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: ~85 mg/mL (~200.7 mM)
Water: <1 mg/mL
Ethanol: ~25 mg/mL (~59.0 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3611 mL 11.8055 mL 23.6111 mL
5 mM 0.4722 mL 2.3611 mL 4.7222 mL
10 mM 0.2361 mL 1.1806 mL 2.3611 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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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.

Biological Data
  • STF-31 inhibits glucose metabolism in VHL-deficient cells. Sci Transl Med . 2011 Aug 3;3(94):94ra70.
  • STF-31 is synthetically lethal to cells dependent on GLUT1 for aerobic glycolysis. Sci Transl Med . 2011 Aug 3;3(94):94ra70.
  • STF-31 has a cell growth inhibition profile similar to that of known NAMPT inhibitors and inhibits recombinant NAMPT. ACS Chem Biol . 2014 Oct 17;9(10):2247-54.
  • Nicotinic acid blocks the effect of STF-31 and other NAMPT inhibitors in NAPRT1-expressing cells. ACS Chem Biol . 2014 Oct 17;9(10):2247-54.
  • NAMPT H191R confers resistance to the growth inhibition effect of STF-31, compound 146, and a known NAMPT inhibitor. ACS Chem Biol . 2014 Oct 17;9(10):2247-54.
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