Primaquine

Name: Primaquine
Brand: MedChemExpress
SKU: HY-12651A
Rating: 5.0 (4 reviews)

Cat. No.: HY-12651A Purity: 98.85%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Primaquine is a potent antimalaria agent and a potent gametocytocide in falciparum malaria. Primaquine prevents relapse in vivax and ovale malaria.

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

Primaquine Chemical Structure

CAS No. : 90-34-6

Size	Price	Stock	Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Oil
50 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 4 publication(s) in Google Scholar

Other Forms of Primaquine:

Primaquine diphosphate In-stock
Primaquine-¹³C,d₃ Get quote

4 Publications Citing Use of MCE Primaquine

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Biological Activity
Purity & Documentation
References
Customer Review

Description

Primaquine is a potent antimalaria agent and a potent gametocytocide in falciparum malaria. Primaquine prevents relapse in vivax and ovale malaria^[1]^[2].

IC₅₀ & Target

Plasmodium

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	> 100 μM Compound: 1, PQ	Cytotoxicity against human A549 cells after 72 hrs Cytotoxicity against human A549 cells after 72 hrs	[PMID: 19799426]
Caco-2	IC₅₀	48 μM Compound: 1	Antitumor activity against human Caco-2 cells after 48 hours hrs by SRB assay Antitumor activity against human Caco-2 cells after 48 hours hrs by SRB assay	[PMID: 19896373]
Hepatocyte	IC₅₀	0.64 μM Compound: Primaquine	Antimalarial activity against Plasmodium yoelii 265 sporozoites in primary mice (Mus musculus) hepatocytes after 48 hrs Antimalarial activity against Plasmodium yoelii 265 sporozoites in primary mice (Mus musculus) hepatocytes after 48 hrs	[PMID: 18456502]
Hepatocyte	CC₅₀	54 μM Compound: PQ	Cytotoxicity against human primary hepatocytes after 48 hrs by MTT assay Cytotoxicity against human primary hepatocytes after 48 hrs by MTT assay	[PMID: 29754074]
Hepatocyte	CC₅₀	54.21 μM Compound: PQ	Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human primary hepatocytes assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30199706]
Hepatocyte	IC₅₀	75.7 nM Compound: Primaquine	Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs Antimicrobial activity against Plasmodium yoelii 265 liver infected in mammalian hepatocytes after 48 hrs	[PMID: 18212104]
HepG2	IC₅₀	< 1 μM Compound: Primaquine	Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin	[PMID: 23927658]
HepG2	IC₅₀	101 μM Compound: PQ	Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay Cytotoxicity against human HepG2 cells after 24 hrs by MTS assay	[PMID: 28939120]
HepG2	IC₅₀	1160 nM Compound: Primaquine	Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis Antiplasmodial activity against liver stage of Plasmodium yoelii 17X NL sporozoites infected in human HepG2 cells expressing CD81 after 48 hrs by DAPI staining-based immunofluorescence analysis	[PMID: 25791675]
HepG2	CC₅₀	120.03 μM Compound: PQ	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30199706]
HepG2	CC₅₀	6.1 μM Compound: Primaquine	Cytotoxicity against human HepG2 cells expressing CD81 assessed as cell viability after 72 hrs by CellTiter-glo assay Cytotoxicity against human HepG2 cells expressing CD81 assessed as cell viability after 72 hrs by CellTiter-glo assay	[PMID: 25791675]
HepG2	CC₅₀	69.8 μM Compound: PQ	Cytotoxicity against human HepG2 cells expressing CD81 assessed as reduction in cell viability after 48 hrs by MTT assay Cytotoxicity against human HepG2 cells expressing CD81 assessed as reduction in cell viability after 48 hrs by MTT assay	[PMID: 30199706]
HT-29	IC₅₀	69.7 μM Compound: 1	Antitumor activity against human HT-29 cells after 48 hours hrs by SRB assay Antitumor activity against human HT-29 cells after 48 hours hrs by SRB assay	[PMID: 19896373]
Huh-7	IC₅₀	2 μM Compound: 1, PQ	Antiplasmodial activity against liver-stage GFP expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as inhibition of parasite schizonts development after 48 hrs by FACS analysis Antiplasmodial activity against liver-stage GFP expressing Plasmodium berghei sporozoites infected in human HuH7 cells assessed as inhibition of parasite schizonts development after 48 hrs by FACS analysis	[PMID: 19799426]
Huh-7	IC₅₀	2.4 μM Compound: 12; PQ	Antimalarial activity against liver stage Plasmodium berghei infected in human Huh-7 cells assessed as inhibition by bioluminescence assay Antimalarial activity against liver stage Plasmodium berghei infected in human Huh-7 cells assessed as inhibition by bioluminescence assay	[PMID: 34242031]
Huh-7	IC₅₀	3.4 μg/mL Compound: Primaquine	Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells assessed as reduction in parasite load treated after 2 hrs of infection for 46 hrs by luciferase assay Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells assessed as reduction in parasite load treated after 2 hrs of infection for 46 hrs by luciferase assay	[PMID: 25103602]
Huh-7	IC₅₀	7.5 μM Compound: Primaquine	Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei expressing luciferase and GFP infected in human HuH7 cells assessed as inhibition of parasite development incubated for 1 hr prior to parasite infection measured after 48 hrs by Antiplasmodial activity against liver sporozoite stage of Plasmodium berghei expressing luciferase and GFP infected in human HuH7 cells assessed as inhibition of parasite development incubated for 1 hr prior to parasite infection measured after 48 hrs by	[PMID: 24125849]
Huh-7	IC₅₀	7.5 μM Compound: 1, PQ	Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay Antiplasmodial activity against liver stage Plasmodium berghei infected in human HuH7 cells co-expressing GFP-Luccon treated for 1 hr prior to infection followed by 24 hrs after compound washout measured after 48 hrs post-infection by Alamar Blue assay	[PMID: 23701465]
Huh-7	IC₅₀	7.5 μM Compound: 3, PQ	Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay Antiplasmodial activity against Plasmodium berghei liver stage form transfected in human Huh-7 cells assessed as cell viability after 48 hrs by luciferase reporter gene assay	[PMID: 23273038]
Huh-7	IC₅₀	7.5 μM Compound: 1, PQ	Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24 Antiplasmodial activity against liver stage of Plasmodium berghei sporozoites expressing firefly luciferase infected in human Huh7 cells assessed as inhibition of parasite development treated 1 hr prior to infection followed by compound replenisment at 24	10.1039/C2MD20113E
Huh-7	IC₅₀	7.5 μM Compound: Primaquine	Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP infected in human Huh7 cells by luminescence assay Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP infected in human Huh7 cells by luminescence assay	[PMID: 23806111]
Huh-7	IC₅₀	7500 nM Compound: 2, PQ	Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells after 48 hrs by luciferase assay Antimalarial activity against liver stage of Plasmodium berghei infected in human Huh7 cells after 48 hrs by luciferase assay	[PMID: 24900781]
Huh-7	IC₅₀	7500 nM Compound: PQ	Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs Antiplasmodial activity against liver stage of Plasmodium berghei infected in human HuH7 cells assessed as parasite growth inhibition incubated for 1 hr prior to parasite infection measured after 48 hrs	[PMID: 24020770]
Huh-7	IC₅₀	8 μM Compound: PQ	Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay Antiplasmodial activity against liver stage of Plasmodium berghei expressing GFP-Luc infected in HuH7 cells incubated at 1 hr prior to infection followed by compound replenisment at 24 hrs post-infection measured after 48 hrs by Alamar blue assay	[PMID: 23290049]
Huh-7	IC₅₀	8.428 μM Compound: PQ	Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay Antiplasmodial activity against liver-stage of Plasmodium berghei expressing firefly luciferase infected in human Huh-7 cells after 48 hrs by bioluminescence assay	[PMID: 26142491]
Huh-7	IC₅₀	9.5 μM Compound: 1	Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay Antiplasmodial activity against liver stage Plasmodium berghei infected in Huh7 cells assessed as inhibition of parasite infection incubated for 1 hr prior to infection measured at 24 hrs by luciferase reporter gene assay	[PMID: 26968650]
MCF7	IC₅₀	6.9 μM Compound: 1	Antitumor activity against human MCF7 cells after 48 hours hrs by SRB assay Antitumor activity against human MCF7 cells after 48 hours hrs by SRB assay	[PMID: 19896373]
RAW264.7	IC₅₀	38.7 μg/mL Compound: 2, PQ	Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay	[PMID: 21141892]
Vero	IC₅₀	≤ 23.8 μg/mL Compound: 1, PQ	Cytotoxicity against African green monkey Vero cells by neutral red uptake assay Cytotoxicity against African green monkey Vero cells by neutral red uptake assay	10.1039/C0MD00267D
Vero	IC₅₀	339.7 μM Compound: PQ, primaquine	Cytotoxicity against african green monkey Vero cells assessed as [3H]hypoxanthine incorporation after 48 hrs Cytotoxicity against african green monkey Vero cells assessed as [3H]hypoxanthine incorporation after 48 hrs	[PMID: 18653332]

In Vitro

Primaquine significantly decreases the cell proliferation of live breast cancer cells, and shows no inhibitory effect on the proliferation of MCF-7 (ER+^{) and MDA-MB-453 (HER}2+^{) cells. Primaquine inhibits the growth, migration, and colony formation of breast cancer cells in vitro^[3].}

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

Cell Viability Assay^[3]

Cell Line:	MDA-MB-231, HCC1937 cells, MCF-7, and MDA-MB-453 cells
Concentration:	5 μM, 10 μM, 20 μM, 40 μM, 80 μM, 100 μM, 120 μM, and 150 μM
Incubation Time:	24 h
Result:	Decreases breast cancer cell viability.

In Vivo

Primaquine (5-25 mg/kg; p.o; daily; for 3 days) demonstrates no bioluminescence liver signal and no blood stage parasitaemia^[2].

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

Animal Model:	Male 6-week-old C57BL/6 albino mice with sporozoite inoculation^[2]
Dosage:	5 mg/kg, 10 mg/kg, 15 mg/kg, 20 mg/kg, and 25 mg/kg
Administration:	p.o; daily; for 3 days
Result:	No blood stage parasitaemia was observed.

Clinical Trial

Molecular Weight

259.35

Formula

C₁₅H₂₁N₃O

CAS No.

90-34-6

Appearance

Oil

Color

Light brown to brown

SMILES

CC(NC1=C2N=CC=CC2=CC(OC)=C1)CCCN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (963.95 mM; Need ultrasonic; 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	3.8558 mL	19.2790 mL	38.5579 mL
5 mM	0.7712 mL	3.8558 mL	7.7116 mL
10 mM	0.3856 mL	1.9279 mL	3.8558 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 (protect from light). 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (8.02 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.85%

Select Batch:

Data Sheet (273 KB) SDS (584 KB)

COA (244 KB) HNMR (274 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Ashley EA, et al. Primaquine: the risks and the benefits. Malar J. 2014 Nov 3;13:418. [Content Brief]

[2]. Qigui Li, et al. Assessment of the prophylactic activity and pharmacokinetic profile of oral tafenoquine compared to primaquine for inhibition of liver stage malaria infections. Malar J. 2014 Apr 14:13:141. [Content Brief]

[3]. Ji-Hyang Kim, et al. Primaquine Inhibits the Endosomal Trafficking and Nuclear Localization of EGFR and Induces the Apoptosis of Breast Cancer Cells by Nuclear EGFR/Stat3-Mediated c-Myc Downregulation. Int J Mol Sci. 2021 Nov 30;22(23):12961. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.8558 mL	19.2790 mL	38.5579 mL	96.3948 mL
	5 mM	0.7712 mL	3.8558 mL	7.7116 mL	19.2790 mL
	10 mM	0.3856 mL	1.9279 mL	3.8558 mL	9.6395 mL
	15 mM	0.2571 mL	1.2853 mL	2.5705 mL	6.4263 mL
	20 mM	0.1928 mL	0.9639 mL	1.9279 mL	4.8197 mL
	25 mM	0.1542 mL	0.7712 mL	1.5423 mL	3.8558 mL
	30 mM	0.1285 mL	0.6426 mL	1.2853 mL	3.2132 mL
	40 mM	0.0964 mL	0.4820 mL	0.9639 mL	2.4099 mL
	50 mM	0.0771 mL	0.3856 mL	0.7712 mL	1.9279 mL
	60 mM	0.0643 mL	0.3213 mL	0.6426 mL	1.6066 mL
	80 mM	0.0482 mL	0.2410 mL	0.4820 mL	1.2049 mL
	100 mM	0.0386 mL	0.1928 mL	0.3856 mL	0.9639 mL

Primaquine 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:

Primaquine90-34-6Parasiteantimalariafalciparum malariagametocytociderelapseInhibitorinhibitorinhibit

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Primaquine

Customer Review

Other Forms of Primaquine:

Primaquine Related Antibodies

4 Publications Citing Use of MCE Primaquine

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•Related Screening Libraries:

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View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Primaquine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Primaquine Related Classifications

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