[CAS NO. 23256-30-6]  Nifurtimox

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PRODUCTS SPECIFICATIONS [23256-30-6]

Catelog
HY-W040073
Brand
MCE
CAS
23256-30-6

DESCRIPTION [23256-30-6]

Overview

MDLMFCD00869254
Molecular Weight287.30
Molecular FormulaC10H13N3O5S
SMILESO=S1(CC(C)N(/N=C/C2=CC=C([N+]([O-])=O)O2)CC1)=O

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

Summary

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] .

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


Clinical Trial

NCT Number Sponsor Condition Start Date Phase
NCT00486564 University of Vermont|St. Louis University
Neuroblastoma
November 2006 Phase 1
NCT01685827 Drugs for Neglected Diseases
Human African Trypanosomiasis (HAT)|Sleeping Sickness
October 2012 Phase 2|Phase 3
NCT00330148 Epicentre|Médecins Sans Frontières, France|Embassy of France in Uganda|National Sleeping Sickness Control Program, Uganda
Trypanosomiasis, African
March 2001 Phase 3

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL ( 522.10 mM ; Need ultrasonic)

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.
In Vivo:
  • 1.

    Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

    Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution

* All of the co-solvents are available by MCE.


Synonyms

4-Thiomorpholinamine, 3-methyl-N-[(5-nitro-2-furanyl)methylene]-, 1,1-dioxide
Thiomorpholine, 3-methyl-4-[(5-nitrofurfurylidene)amino]-, 1,1-dioxide
3-Methyl-4-(5-nitrofurfurylideneamino)tetrahydro-1,4-thiazine-1,1-dioxide
BAY 2502
Bayer 2502
Tetrahydro-3-methyl-4-[(5-nitrofurfurylidene)amino]-4H-1,4-thiazine 1,1-dioxide
Nifurtimox
Lampit
4-(5-Nitrofurfurylideneamino)-3-methylthiomorpholine 1,1-dioxide
(±)-Nifurtimox
BAY-A 2502