1. Anti-infection
    Metabolic Enzyme/Protease
  2. Parasite
    Lactate Dehydrogenase

Nifurtimox 

Cat. No.: HY-W040073
Handling Instructions

Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

For research use only. We do not sell to patients.

Nifurtimox Chemical Structure

Nifurtimox Chemical Structure

CAS No. : 23256-30-6

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).

IC50 & Target

Trypanosoma cruzi[1]
Lactate dehydrogenase (LDH) [1]

In Vitro

Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH). To differentiate if this effect is a result of a reduced LDH activity or a shift in pyruvate metabolism due to activation of PDH, the enzyme activity of LDH is determined after 4 h treatment with 50 µg/mL Nifurtimox. Compared to the untreated control, the LDH activity is significantly reduced for LA-N-1 (P=0.005), IMR-32 (P=0.009), LS (P=0.0035) and SK-N-SH (P=0.0065). Nifurtimox reduces cell viability and induces cell cycle arrest and apoptosis in neuroblastoma cells. To characterize the cytotoxic impacts of Nifurtimox on neuroblastoma, 4 cell lines are subjected to several experiments. Cell viability is reduced for all 4 neuroblastoma cell lines after 24 h incubation with 50 µg/mL to an average of 66%, 63%, 62% and 75% (LA-N-1, IMR-32 LS and SK-N-SH, respectively). The reduction is significant compared to the untreated control (P<0.01) and the vehicle control with DMSO (P<0.05) for all cell lines[1].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.4807 mL 17.4034 mL 34.8068 mL
5 mM 0.6961 mL 3.4807 mL 6.9614 mL
10 mM 0.3481 mL 1.7403 mL 3.4807 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

The Neuroblastoma cell lines IMR-32, LA-N-1 and SK-N-SH and the neuroblastoma cell line LS are grown in RPMI-1640 medium supplemented with 10% (v/v) fetal calf serum (FCS), 2 mM L-glutamine, 100 U/mL Penicillin and 100 µg/mL Streptomycin and incubated at 37°C, 5% CO2 and saturated humidity. To assess the cell viability after incubation with Nifurtimox at different concentrations (10 µg/mL up to 50 µg/mL or 34.8 µM to 174 µM, respectively in the supernatant growth medium) or the vehicle control with according concentrations, all neuroblastoma cell lines are subjected to an MTS assay. Stock solutions of MTS are made at 480 µM in sterile filtered deionized water and stored at -20°C. Cells are grown to approximately 50% confluency, treated with Nifurtimox, and incubated for 1 h with fresh media containing 12 µM MTS[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

287.30

Formula

C₁₀H₁₃N₃O₅S

CAS No.

23256-30-6

SMILES

O=S1(CC(C)N(/N=C/C2=CC=C([N+]([O-])=O)O2)CC1)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Nifurtimox
Cat. No.:
HY-W040073
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Nifurtimox

Cat. No.: HY-W040073