Melarsoprol

Cat. No.: HY-119594 Purity: 98.0%: Data Sheet
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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.

Melarsoprol Chemical Structure

CAS No. : 494-79-1

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
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	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	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	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	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	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	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	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	19000 nM 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	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	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	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	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	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	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	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 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 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells after 70 hrs by Alamar blue assay	[PMID: 33148495]
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	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	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	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 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: 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	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	7.78 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	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: 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	7.8 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	7.9 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]
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]

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

Molecular Weight

398.34

Formula

C₁₂H₁₅AsN₆OS₂

CAS No.

494-79-1

Appearance

Solid

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 98.0%

Select Batch:

Data Sheet (273 KB) SDS (564 KB)

COA (246 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]

Complete Stock Solution Preparation Table

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

Melarsoprol Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Melarsoprol494-79-1ParasiteApoptosisMelaminophenylarsinetrivalent organic arsenicalAfrican trypanosomiasisleukemia cellplasma cellmyelomaGSHInhibitorinhibitorinhibit

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