Cat. No.: HY-W040073

Nifurtimox

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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.

Purity: 99.72%
CAS No.: 23256-30-6
Formula: C₁₀H₁₃N₃O₅S
Molecular Weight:287.30

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Nifurtimox Chemical Structure

CAS No.: 23256-30-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
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Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

Trypanosoma

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	GI₅₀	13.9 μg/mL Compound: nifurtimox	Cytotoxicity against CHO cells assessed as cell viability after 48 hrs by MTT colorimetric assay Cytotoxicity against CHO cells assessed as cell viability after 48 hrs by MTT colorimetric assay	[PMID: 22551062]
Fibroblast	IC₅₀	>200 μM Compound: NFX	Cytotoxicity against human fibroblasts assessed as growth inhibition after 24 hrs by MTT assay Cytotoxicity against human fibroblasts assessed as growth inhibition after 24 hrs by MTT assay	[PMID: 23644203]
H9c2	IC₅₀	>50 μM Compound: Nifurtimox	Cytotoxicity against rat H9c2 cells infected with Trypanosoma cruzi Tulahuen amastigote forms assessed as reduction in cell number after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis Cytotoxicity against rat H9c2 cells infected with Trypanosoma cruzi Tulahuen amastigote forms assessed as reduction in cell number after 72 hrs by DRAQ5 DNA dye based confocal microscopic analysis	[PMID: 30100019]
HEK293	EC₅₀	>100 μM Compound: Nifurtimox	Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by alamar blue assay	[PMID: 27720295]
HeLa	IC₅₀	12 μM Compound: Nfx	Cytotoxicity against human HeLa cells after 24 hrs by MTT assay Cytotoxicity against human HeLa cells after 24 hrs by MTT assay	[PMID: 19168363]
HeLa	EC₅₀	91.2 μM Compound: 5	Cytotoxicity against human HeLa cells after 65 hrs by Alamar blue assay Cytotoxicity against human HeLa cells after 65 hrs by Alamar blue assay	[PMID: 23281892]
HeLa	EC₅₀	272 μM Compound: Nfx	Cytotoxicity against human HeLa cells measured after 24 hrs by crystal violet staining based assay Cytotoxicity against human HeLa cells measured after 24 hrs by crystal violet staining based assay	[PMID: 27810595]
HepG2	CC₅₀	45.2 μM Compound: Nifurtimox	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32652409]
HepG2	CC₅₀	45.2 μM Compound: Nifurtimox	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32795774]
IMR-90	EC₅₀	>25 μM Compound: Nifurtimox	Cytotoxicity against human IMR90 cells after 44 to 46 hrs by CellTiter-Blue assay Cytotoxicity against human IMR90 cells after 44 to 46 hrs by CellTiter-Blue assay	[PMID: 28119024]
J774	IC₅₀	>200 μM Compound: S5	Cytotoxicity against J774.1 cell line after 48 hrs Cytotoxicity against J774.1 cell line after 48 hrs	[PMID: 16516467]
J774	IC₅₀	316 μM Compound: Nfx	Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 23811257]
J774	IC₅₀	280.48 μM Compound: NFX	Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells after 48 hrs by MTT assay	[PMID: 23816040]
J774	IC₅₀	316 μM Compound: Nfx	Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 25008454]
J774	IC₅₀	7 μM Compound: Nfx	Trypanocidal activity against Trypanosoma cruzi Y epimastigotes infected in mouse J774 cells assessed as growth inhibition of parasite measured on day 5 Trypanocidal activity against Trypanosoma cruzi Y epimastigotes infected in mouse J774 cells assessed as growth inhibition of parasite measured on day 5	[PMID: 25008454]
J774	CC₅₀	131.503 μM Compound: NFX	Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin assay Cytotoxicity against mouse J774 cells assessed as decrease in cell viability after 24 hrs by resazurin assay	[PMID: 27503677]
J774	IC₅₀	316 μM Compound: Nifurtimox	Cytotoxicity against mouse J774 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against mouse J774 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 28499168]
J774	CC₅₀	131.5 μM Compound: Nfx	Cytotoxicity against mouse J774 cells incubated for 24 hrs by resazurin dye based fluorescence assay Cytotoxicity against mouse J774 cells incubated for 24 hrs by resazurin dye based fluorescence assay	[PMID: 28648464]
J774	EC₅₀	150 μM Compound: Nfx	Cytotoxicity against mouse J774 cells assessed as reduction in cell viability after 24 hrs by WST-1 assay Cytotoxicity against mouse J774 cells assessed as reduction in cell viability after 24 hrs by WST-1 assay	[PMID: 31673311]
J774	CC₅₀	100 μM Compound: Nifurtimox	Cytotoxicity against mouse J774 cells after 24 hrs by WST-1 assay Cytotoxicity against mouse J774 cells after 24 hrs by WST-1 assay	[PMID: 36508970]
J774.2	CC₅₀	164.2 μM Compound: Nfx	Cytotoxicity against mouse J774.2 cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based assay Cytotoxicity against mouse J774.2 cells assessed as reduction in cell viability measured after 48 hrs by resazurin dye based assay	[PMID: 34571489]
J774.A1	CC₅₀	201.1 μM Compound: Nfx	Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability measured after 20 hrs by MTT assay Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability measured after 20 hrs by MTT assay	[PMID: 30784876]
L6	IC₅₀	68 μM Compound: nifurtimox	Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts Concentration causing cytotoxicity to 50% of L-6 rat skeletal myoblasts	[PMID: 16107157]
L6	CC₅₀	78.2 μM Compound: Nifurtimox	Cytotoxicity against rat L6 cells after 5 days by resazurin assay Cytotoxicity against rat L6 cells after 5 days by resazurin assay	[PMID: 25089808]
L6	IC₅₀	32 μM Compound: nifurtimox	Cytotoxicity against rat L6 cells after 6 days by resazurin staining based fluorescence plate reader assay Cytotoxicity against rat L6 cells after 6 days by resazurin staining based fluorescence plate reader assay	[PMID: 26479031]
L6	IC₅₀	32 μM Compound: Nifurtimox	Cytotoxicity against rat L6 cells after 6 days by resazurin based fluorescence assay Cytotoxicity against rat L6 cells after 6 days by resazurin based fluorescence assay	[PMID: 27591008]
L929	IC₅₀	>256 μM Compound: Nifurtimox	Cytotoxicity against mouse NCTC-929 cells assessed as reduction in cell viability after 48 hrs by resazurin dye-based assay Cytotoxicity against mouse NCTC-929 cells assessed as reduction in cell viability after 48 hrs by resazurin dye-based assay	[PMID: 28499168]
LLC-MK2	IC₅₀	1.9 μM Compound: Nfx	Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 11 days Antitrypanosomal activity against epimastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 11 days	[PMID: 23167554]
LLC-MK2	IC₅₀	2.7 μM Compound: Nfx	Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 24 hrs Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi Y infected in LLC-MK2 cells assessed as parasite motility after 24 hrs	[PMID: 23167554]
LLC-MK2	CC₅₀	2.7 μM Compound: Nfx	Antitrypanosomal activity against Trypanosoma cruzi Y metacyclic trypomastigotes isolated from infected LLC-MK2 cells assessed as parasite viability after 24 hrs by neubauer chamber analysis Antitrypanosomal activity against Trypanosoma cruzi Y metacyclic trypomastigotes isolated from infected LLC-MK2 cells assessed as parasite viability after 24 hrs by neubauer chamber analysis	[PMID: 24561675]
MRC5	CC₅₀	>50 μM Compound: Nifurtimox	Tested for cytotoxicity towards human MRC-5 cells Tested for cytotoxicity towards human MRC-5 cells	[PMID: 12443785]
MRC5	IC₅₀	0.7 μM Compound: Nifurtimox	Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay	[PMID: 25199582]
NIH3T3	IC₅₀	3 μg/mL Compound: nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells assessed as beta-galactosidase activity after 7 days by chagas bioassay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells assessed as beta-galactosidase activity after 7 days by chagas bioassay	[PMID: 20441198]
RAW264.7	IC₅₀	263.44 μM Compound: Nifurtimox	Cytotoxicity against mouse RAW264.7 cells measured after 4 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells measured after 4 hrs by MTT assay	[PMID: 27908757]
THP-1	IC₅₀	64.8 μM Compound: nifurtimox	Cytotoxicity against human THP1 cells after 6 days by Alamar blue assay Cytotoxicity against human THP1 cells after 6 days by Alamar blue assay	[PMID: 20028822]
THP-1	IC₅₀	>100 μM Compound: Nifurtimox	Cytotoxicity against human THP1 cells by AlamarBlue assay Cytotoxicity against human THP1 cells by AlamarBlue assay	[PMID: 24119553]
U2OS	CC₅₀	97.2 μM Compound: Nifurtimox	Cytotoxicity against human U2OS cells assessed as reduction in cell viability Cytotoxicity against human U2OS cells assessed as reduction in cell viability	[PMID: 26774924]
U2OS	EC₅₀	1.26 μM Compound: Nifurtimox	Antiparasitic activity against Trypanosoma cruzi Y trypomastigotes infected in rhesus monkey LLC-MK2 cells followed by re-infection of amastigotes in human U2OS cells assessed as reduction in parasite infection level after 96 hrs by draq5 staining based a Antiparasitic activity against Trypanosoma cruzi Y trypomastigotes infected in rhesus monkey LLC-MK2 cells followed by re-infection of amastigotes in human U2OS cells assessed as reduction in parasite infection level after 96 hrs by draq5 staining based a	[PMID: 26774924]
U2OS	CC₅₀	26.8 μM Compound: Nifurtimox	Cytotoxicity against human U2OS cells infected with amastigote stage of Trypanosoma cruzi Y assessed as decrease in number of cells after 96 hrs by Draq5 staining-based high content screening assay Cytotoxicity against human U2OS cells infected with amastigote stage of Trypanosoma cruzi Y assessed as decrease in number of cells after 96 hrs by Draq5 staining-based high content screening assay	[PMID: 27318979]
U2OS	EC₅₀	0.34 μM Compound: Nifurtimox	Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Y infected in human U2OS cells after 96 hrs by Draq5 staining-based high content screening assay Antitrypanosomal activity against amastigote stage of Trypanosoma cruzi Y infected in human U2OS cells after 96 hrs by Draq5 staining-based high content screening assay	[PMID: 27318979]
U2OS	CC₅₀	85.19 μM Compound: NFX	Cytotoxicity against human U2OS cells assessed as reduction in cell viability Cytotoxicity against human U2OS cells assessed as reduction in cell viability	[PMID: 29247858]
V79	IC₅₀	146 μM Compound: Nifurtimox	Therapeutic index, ratio of IC50 for chinese hamster V79 cells to IC50 for Trypanosoma cruzi Therapeutic index, ratio of IC50 for chinese hamster V79 cells to IC50 for Trypanosoma cruzi	[PMID: 20679506]
V79	IC₅₀	17 μM Compound: Nifurtimox	Therapeutic index, ratio of IC50 for chinese hamster V79 cells to IC50 for Trypanosoma brucei BSF Therapeutic index, ratio of IC50 for chinese hamster V79 cells to IC50 for Trypanosoma brucei BSF	[PMID: 20679506]
V79	IC₅₀	35 μM Compound: Nifurtimox	Cytotoxicity against chinese hamster V79 cells after 6 days by Alamar blue assay Cytotoxicity against chinese hamster V79 cells after 6 days by Alamar blue assay	[PMID: 20679506]
Vero	IC₅₀	11 μM Compound: Nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 infected in african green monkey Vero cells assessed as growth inhibition of trypomastigotes by beta-galactosidase reporter gene assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 infected in african green monkey Vero cells assessed as growth inhibition of trypomastigotes by beta-galactosidase reporter gene assay	[PMID: 17067146]
Vero	IC₅₀	10 μM Compound: nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in vero cells assessed as intracellular growth inhibition of trypomastigote by beta-galactosidase reporter gene assay Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in vero cells assessed as intracellular growth inhibition of trypomastigote by beta-galactosidase reporter gene assay	[PMID: 18715036]
Vero	IC₅₀	0.52 μM Compound: Nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in african green monkey Vero cells after 120 hrs Antitrypanosomal activity against Trypanosoma cruzi Tulahuen C4 in african green monkey Vero cells after 120 hrs	[PMID: 18798609]
Vero	IC₅₀	80.1 μM Compound: Nifurtimox	Cytotoxicity against african green monkey Vero cells by MTT assay Cytotoxicity against african green monkey Vero cells by MTT assay	[PMID: 18798609]
Vero	CC₅₀	113.6 μM Compound: Nfx	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 19321339]
Vero	IC₅₀	1.4 μM Compound: Nfx	Antiparasitic activity against Trypanosoma cruzi 320I04 intracellular amastigotes infected in african green monkey Vero cells after 72 hrs Antiparasitic activity against Trypanosoma cruzi 320I04 intracellular amastigotes infected in african green monkey Vero cells after 72 hrs	[PMID: 19321339]
Vero	IC₅₀	4.8 μM Compound: Nfx	Antiparasitic activity against Trypanosoma cruzi 320I04 epimastigotes infected in african green monkey Vero cells after 72 hrs Antiparasitic activity against Trypanosoma cruzi 320I04 epimastigotes infected in african green monkey Vero cells after 72 hrs	[PMID: 19321339]
Vero	IC₅₀	13.5 μM Compound: Nifurtimox	Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 infected african green monkey Vero cells expressing beta-galctosidase after 5 days Antiparasitic activity against Trypanosoma cruzi Tulahuen C4 infected african green monkey Vero cells expressing beta-galctosidase after 5 days	[PMID: 20030365]
Vero	IC₅₀	4.5 μM Compound: Nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi tulahuen C4 trypomastigotes infected in african green monkey Vero cells assessed as CPRG cleavage after 120 hrs by microplate reader Antitrypanosomal activity against Trypanosoma cruzi tulahuen C4 trypomastigotes infected in african green monkey Vero cells assessed as CPRG cleavage after 120 hrs by microplate reader	[PMID: 20356752]
Vero	IC₅₀	94 μM Compound: Nifurtimox	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay	[PMID: 20356752]
Vero	CC₅₀	61.42 μM Compound: Nfx	Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay	[PMID: 20627590]
Vero	IC₅₀	2.3 μM Compound: Nfx	Antitrypanosomal activity against Trypanosoma cruzi 320I01 amastigotes infected in african green monkey Vero cells after 5 days by Giemsa staining Antitrypanosomal activity against Trypanosoma cruzi 320I01 amastigotes infected in african green monkey Vero cells after 5 days by Giemsa staining	[PMID: 20627590]
Vero	IC₅₀	0.24 μM Compound: Nifurtimox	Antitrypanosomal activity against Trypanosoma cruzi clone Cl-Brener infected in african green monkey Vero cells assessed as growth inhibition after 3 days by luciferase reporter gene assay Antitrypanosomal activity against Trypanosoma cruzi clone Cl-Brener infected in african green monkey Vero cells assessed as growth inhibition after 3 days by luciferase reporter gene assay	[PMID: 20679506]
Vero	IC₅₀	64.11 μM Compound: Nifurtimox	Cytotoxicity against african green monkey Vero cells after 6 days by Alamar blue assay Cytotoxicity against african green monkey Vero cells after 6 days by Alamar blue assay	[PMID: 20679506]
Vero	IC₅₀	10.4 μM Compound: Nfx	Trypanosomicidal activity against amastigote stage of Trypanosoma cruzi Tulahuen C4 transfected with beta-D-galactosidase infected in african green monkey Vero cells assessed as growth inhibition incubated 5 days prior to beta-D-galactopyranoside addition Trypanosomicidal activity against amastigote stage of Trypanosoma cruzi Tulahuen C4 transfected with beta-D-galactosidase infected in african green monkey Vero cells assessed as growth inhibition incubated 5 days prior to beta-D-galactopyranoside addition	[PMID: 23202852]
Vero	IC₅₀	21.05 μM Compound: Nifurtimox	Trypanocidal activity against epimastigote stage of Trypanosoma cruzi infected in african green monkey Vero cells assessed as cell viability after 24 hrs by MTT assay Trypanocidal activity against epimastigote stage of Trypanosoma cruzi infected in african green monkey Vero cells assessed as cell viability after 24 hrs by MTT assay	[PMID: 25127463]
Vero	IC₅₀	411.13 μM Compound: Nifurtimox	Cytotoxicity against african green monkey Vero cells by MTT assay Cytotoxicity against african green monkey Vero cells by MTT assay	[PMID: 25127463]
Vero	CC₅₀	67.5 μM Compound: Nfx	Cytotoxicity against African green monkey Vero cells Cytotoxicity against African green monkey Vero cells	[PMID: 25173828]
Vero	IC₅₀	1.6 μM Compound: Nfx	Antiparasitic activity against amastigote stage of Trypanosoma cruzi infected in Vero cells assessed as parasite growth inhibition after 24 hrs by hemocytometery Antiparasitic activity against amastigote stage of Trypanosoma cruzi infected in Vero cells assessed as parasite growth inhibition after 24 hrs by hemocytometery	[PMID: 25173828]
Vero	IC₅₀	4 μM Compound: Nfx	Antiparasitic activity against epimastigote stage of Trypanosoma cruzi infected in Vero cells assessed as parasite growth inhibition after 24 hrs by hemocytometery Antiparasitic activity against epimastigote stage of Trypanosoma cruzi infected in Vero cells assessed as parasite growth inhibition after 24 hrs by hemocytometery	[PMID: 25173828]
Vero	CC₅₀	163 μM Compound: Nfx, Lampit	Cytotoxicity against African green monkey Vero cells after 24 hrs by MTT assay Cytotoxicity against African green monkey Vero cells after 24 hrs by MTT assay	[PMID: 25899334]
Vero	IC₅₀	10 μM Compound: Nifurtimox	Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Dm28c infected in African green monkey Vero cells assessed as growth inhibition incubated for 5 to 7 days post infection measured after 24 hrs by MTT assay Antitrypanosomal activity against trypomastigote stage of Trypanosoma cruzi Dm28c infected in African green monkey Vero cells assessed as growth inhibition incubated for 5 to 7 days post infection measured after 24 hrs by MTT assay	[PMID: 27908757]
Vero	CC₅₀	32 μM Compound: Nifurtimox	Cytotoxicity against African green monkey Vero cells incubated for 24 to 48 hrs by SRB assay Cytotoxicity against African green monkey Vero cells incubated for 24 to 48 hrs by SRB assay	[PMID: 28645659]
Vero	EC₅₀	50 μM Compound: NF	Cytotoxic activity against African green monkey Vero cells Cytotoxic activity against African green monkey Vero cells	[PMID: 29748049]
Vero	IC₅₀	115 μM Compound: NFX	Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay	[PMID: 30344907]

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].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 23256-30-6
Appearance Solid
Molecular Weight 287.30
Formula C₁₀H₁₃N₃O₅S
Color Light yellow to yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Int J Biol Macromol

Reticuline isomerase AKR1B1 with aldo-keto reductase activity and detoxification function from the insect Blaps rhynchopetera. [Abstract]

2026 Mar:352:151224. PMID: 41791543

Solvent & Solubility

In Vitro:

DMSO : 150 mg/mL (522.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Concentration Solvent Mass

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Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

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].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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OR (2659 KB)
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Handling Instructions (2659 KB)

References

[1]. Cabanillas Stanchi KM, et al. Nifurtimox reduces N-Myc expression and aerobic glycolysis in neuroblastoma. Cancer Biol Ther. 2015;16(9):1353-63. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.4807 mL	17.4034 mL	34.8068 mL	87.0171 mL
	5 mM	0.6961 mL	3.4807 mL	6.9614 mL	17.4034 mL
	10 mM	0.3481 mL	1.7403 mL	3.4807 mL	8.7017 mL
	15 mM	0.2320 mL	1.1602 mL	2.3205 mL	5.8011 mL
	20 mM	0.1740 mL	0.8702 mL	1.7403 mL	4.3509 mL
	25 mM	0.1392 mL	0.6961 mL	1.3923 mL	3.4807 mL
	30 mM	0.1160 mL	0.5801 mL	1.1602 mL	2.9006 mL
	40 mM	0.0870 mL	0.4351 mL	0.8702 mL	2.1754 mL
	50 mM	0.0696 mL	0.3481 mL	0.6961 mL	1.7403 mL
	60 mM	0.0580 mL	0.2901 mL	0.5801 mL	1.4503 mL
	80 mM	0.0435 mL	0.2175 mL	0.4351 mL	1.0877 mL
	100 mM	0.0348 mL	0.1740 mL	0.3481 mL	0.8702 mL

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Nifurtimox

Anti-Infection Compound Library

Metabolism/Protease Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Glycolysis Compound Library

FDA Approved & Pharmacopeial Drug Library

Antiparasitic Compound library

Anti-Cancer Metabolism Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Rare Diseases Drug Library

Pediatric Drug Library

FDA-Approved Anticancer Drug Library

Heterocyclic Compound Library

Off-patent Drug Library

Metabolic Enzyme Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Lactic Acid Metabolic Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

3D Diverse Fragment Library

Publications Citing Use of MedChemExpress (MCE) Nifurtimox

All Parasite Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Nifurtimox Related Classifications

HY-W040073 Related Classifications