Cat. No.: HY-119594

Melarsoprol

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Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important agent for African trypanosomiasis. Melarsoprol inhibits the growth of lymphoid leukemic cell by inducing apoptosis. Melarsoprol crosses the blood-brain barrier.

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

Purity: 98.0%
CAS No.: 494-79-1
Formula: C₁₂H₁₅AsN₆OS₂
Molecular Weight:398.34

Storage:

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

Melarsoprol Chemical Structure

CAS No.: 494-79-1

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
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Biological Activity

Description

All Parasite Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	EC₅₀	4270 nM Compound: melarsoprol	Cytotoxicity against human HL60 cells Cytotoxicity against human HL60 cells	[PMID: 17371810]
HT-29	IC₅₀	3.6 μg/mL Compound: Melarsoprol	Cytotoxicity against human HT-29 cells Cytotoxicity against human HT-29 cells	[PMID: 9599255]
J774	IC₅₀	4.3 μM Compound: S4	Cytotoxicity against J774.1 cell line after 48 hrs Cytotoxicity against J774.1 cell line after 48 hrs	[PMID: 16516467]
L6	IC₅₀	7.8 μM Compound: Melarsoprol	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	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against L6 cells Cytotoxicity against L6 cells	[PMID: 16889962]
L6	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against rat L6 cells after 72 hrs by microplate assay Cytotoxicity against rat L6 cells after 72 hrs by microplate assay	[PMID: 17544672]
L6	IC₅₀	7.78 μM Compound: Mel, melarsoprol	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 17698258]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 17948982]
L6	IC₅₀	7.78 μM Compound: melarsoprol (mel)	Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by microplate alamar blue assay	[PMID: 18502136]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 18841956]
L6	IC₅₀	7.78 μM Compound: MAP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19267462]
L6	IC₅₀	7.78 μM Compound: Mel	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 19395265]
L6	IC₅₀	7.8 μM Compound: MLSP	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 19409677]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19606902]
L6	IC₅₀	8.6 μM Compound: melarsoprol	Toxicity against rat L6 cells Toxicity against rat L6 cells	[PMID: 19781948]
L6	IC₅₀	7.78 μM Compound: MLSP	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 19928900]
L6	IC₅₀	0.008 μM Compound: Melarsoprol	Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in rat L6 cells Antitrypanosomal activity against Trypanosoma brucei rhodesiense infected in rat L6 cells	[PMID: 19942439]
L6	IC₅₀	7.9 μM Compound: MLS	Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by alamar blue assay	[PMID: 20047276]
L6	IC₅₀	7.78 μM Compound: 25	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 20303767]
L6	IC₅₀	1.3 μg/mL Compound: Melarsoprol	Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay Cytotoxicity against in rat L6 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay	[PMID: 21353728]
L6	IC₅₀	0.013 μM Compound: Melarsoprol	Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay Antiparasitic activity against bloodstream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 21937228]
L6	IC₅₀	0.01 μM Compound: Melarsoprol	Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against blood stream form of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22023653]
L6	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 22136906]
L6	IC₅₀	0.005 μg/mL Compound: Melarsoprol	Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against trypomastigotes of Trypanosoma brucei rhodesiense STIB 900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22352841]
L6	EC₅₀	0.0075 μM Compound: melarsoprol	Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay	[PMID: 22390399]
L6	IC₅₀	18.3 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by inverted microscopy	[PMID: 23153330]
L6	IC₅₀	5.12 μM Compound: MSP, MLSP	Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar Blue assay	[PMID: 23795673]
L6	IC₅₀	7.78 mM Compound: MLSP	Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by Alamar blue assay	[PMID: 23871911]
L6	IC₅₀	7.78 μM Compound: Mel	Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorometry	[PMID: 23880082]
L6	IC₅₀	5.12 μM Compound: MSP	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by Alamar blue assay	[PMID: 24268543]
L6	IC₅₀	19 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay Cytotoxicity against rat L6 cells assessed as cell viability after 70 hrs by MTT assay	[PMID: 24398295]
L6	IC₅₀	0.008 μM Compound: Melarsoprol	Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay Antimicrobial activity against trypomastigote stage of Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 96 hrs by Alamar Blue assay	[PMID: 24865793]
L6	IC₅₀	5.1 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay Cytotoxicity against rat L6 cells after 3 days by Alamar blue assay	[PMID: 24956553]
L6	IC₅₀	29.1 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells Cytotoxicity against rat L6 cells	[PMID: 25740635]
L6	IC₅₀	7.78 μM Compound: Ml	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 25746816]
L6	IC₅₀	18.3 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells after 72 hrs by alamar blue assay	[PMID: 26237241]
L6	IC₅₀	5.12 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis Cytotoxicity against rat L6 cells measured after 70 hrs by alamar blue staining based fluorescence analysis	[PMID: 27102161]
L6	IC₅₀	7.78 μM Compound: MEL	Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 72 hrs by Alamar blue assay	[PMID: 27344215]
L6	IC₅₀	7.78 μM Compound: MEL	Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay Cytotoxicity against rat L6 cells assessed as growth inhibition after 70 hrs by alamar blue assay	[PMID: 28031151]
L6	IC₅₀	29 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay Cytotoxicity against rat L6 cells assessed as growth inhibition after 72 hrs by alamar blue assay	[PMID: 28284860]
L6	CC₅₀	28.9 μM Compound: MEL	Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis Cytotoxicity against rat L6 cels assessed as reduction in cell viability after 72 hrs by Alamar Blue dye-based fluorometric analysis	[PMID: 30615444]
L6	IC₅₀	24.2 μM Compound: Melarsoprol	Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis Cytotoxicity against rat L6 cells assessed as reduction in cell viability measured after 72 hrs by Alamar blue based inverted microscopy analysis	[PMID: 31784198]
L6	IC₅₀	7.78 μM Compound: mel	Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay	[PMID: 33148495]
MRC5	CC₅₀	12.5 μM Compound: Melarsoprol	In Vitro cytotoxicity on MRC-5 cells In Vitro cytotoxicity on MRC-5 cells	[PMID: 10893302]
MRC5	CC₅₀	12.5 μM Compound: Melarsoprol	Tested for cytotoxicity towards human MRC-5 cells Tested for cytotoxicity towards human MRC-5 cells	[PMID: 12443785]
MRC5	IC₅₀	7.4 μM Compound: Melarsoprol	Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs Cytotoxicity against human MRC5 SV2 cells assessed as reduction in cell growth after 72 hrs	[PMID: 25199582]
MRC5	IC₅₀	12.5 μM Compound: Mel	Cytotoxicity against human MRC5 cells incubated for 7 days by MTT colorimetric assay Cytotoxicity against human MRC5 cells incubated for 7 days by MTT colorimetric assay	[PMID: 37084599]

In Vitro

Melarsoprol (1-100 nM; 24-96 h) causes a dose- and time-dependent inhibition of survival and growth in lymphoid leukemic cells^[2].
Melarsoprol (10-100 nM; 24 h) exhibits morphologic characteristics of apoptosis^[2].
Melarsoprol (1-100 nM; 24 h) inhibits the expression of bcl-2 mRNA and protein^[2].

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

Cell Viability Assay^[2]

Cell Line:

An Epstein-Barr virus (EBV)-transformed B-prolymphocytic cell line (JVM-2), an EBV-transformed B-cell chronic lymphocytic leukemia (B-CLL) cell line (I83CLL), and one non-EBV-transformed B-CLL cell line (WSU-CLL)
Concentration:

1 nM, 10 nM, 100 nM
Incubation Time:

24 h, 48 h, 96 h
Result:

Caused a dose- and time-dependent inhibition of survival and growth in all three cell lines.

Apoptosis Analysis^[2]

Cell Line:

WSU-CLL, I83CLL and JVM-2 cells
Concentration:

10 nM, 100 nM
Incubation Time:

24 h
Result:

Showed characteristic apoptotic changes, such as chromatin condensation and fragmentation, membrane blebbing, and formation of apoptotic bodies.

RT-PCR^[2]

Cell Line:

WSU-CLL, I83CLL and JVM-2 cells
Concentration:

10 nM, 100 nM
Incubation Time:

24 h
Result:

Observed prominent concentration-dependent downregulation of bcl-2 mRNA.

Western Blot Analysis^[2]

Cell Line:

WSU-CLL, I83CLL and JVM-2 cells
Concentration:

1 nM, 110 nM, 100 nM
Incubation Time:

24 h
Result:

Decrease of bcl-2 protein expression was observed.

In Vivo

In mice, the organic solution of Melarsoprol (0.039 mmol/kg), injected intravenously as control formulation, is found to concentrate significantly in the bone marrow (C_max = 1.64 mmol/g), though, the brain concentration is quite high (C_max = 0. 093 mmol/g) and the LD₅₀ is 0.12 mmol/kg^[3].

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. 494-79-1
Appearance Solid
Molecular Weight 398.34
Formula C₁₂H₁₅AsN₆OS₂
Color White to off-white
SMILES

OCC1S[As](SC1)C2=CC=C(C=C2)NC3=NC(N)=NC(N)=N3
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 : 36 mg/mL (90.38 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5104 mL

12.5521 mL

25.1042 mL

5 mM

0.5021 mL

2.5104 mL

5.0208 mL

10 mM

0.2510 mL

1.2552 mL

2.5104 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (624 KB)
- English - EN (624 KB)
- Français - FR (624 KB)
- Deutsch - DE (624 KB)
- Norwegian - NO (624 KB)
- Español - ES (624 KB)
- Swedish - SV (624 KB)
- Italian - IT (624 KB)
- Korean - KR (624 KB)
- Portuguese - PT (624 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Z Gregus, et al. Role of glutathione in the biliary excretion of the arsenical drugs trimelarsan and melarsoprol. Biochem Pharmacol. 2000 Jun 1;59(11):1375-85. [Content Brief]

[2]. König A, et al. Comparative activity of melarsoprol and arsenic trioxide in chronic B-cell leukemia lines. Blood. 1997 Jul 15;90(2):562-70. [Content Brief]

[3]. Ben Zirar S, et al. Comparison of nanosuspensions and hydroxypropyl-beta-cyclodextrin complex of melarsoprol: pharmacokinetics and tissue distribution in mice. Eur J Pharm Biopharm. 2008 Oct;70(2):649-56. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5104 mL	12.5521 mL	25.1042 mL	62.7605 mL
	5 mM	0.5021 mL	2.5104 mL	5.0208 mL	12.5521 mL
	10 mM	0.2510 mL	1.2552 mL	2.5104 mL	6.2760 mL
	15 mM	0.1674 mL	0.8368 mL	1.6736 mL	4.1840 mL
	20 mM	0.1255 mL	0.6276 mL	1.2552 mL	3.1380 mL
	25 mM	0.1004 mL	0.5021 mL	1.0042 mL	2.5104 mL
	30 mM	0.0837 mL	0.4184 mL	0.8368 mL	2.0920 mL
	40 mM	0.0628 mL	0.3138 mL	0.6276 mL	1.5690 mL
	50 mM	0.0502 mL	0.2510 mL	0.5021 mL	1.2552 mL
	60 mM	0.0418 mL	0.2092 mL	0.4184 mL	1.0460 mL
	80 mM	0.0314 mL	0.1569 mL	0.3138 mL	0.7845 mL

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Melarsoprol

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Antiparasitic Compound library

Rare Diseases Drug Library

Pediatric Drug Library

Cell Death Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All Parasite Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Melarsoprol

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

Apoptosis Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

Antiparasitic Compound library

Rare Diseases Drug Library

Pediatric Drug Library

Cell Death Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

All Parasite Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Melarsoprol Related Classifications

HY-119594 Related Classifications