Primaquine diphosphate (Synonyms: Primaquine phosphate; Primaquine bisphosphate)

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

Cat. No.: HY-12651 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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

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

Primaquine diphosphate Chemical Structure

CAS No. : 63-45-6

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10 mM * 1 mL in DMSO ready for reconstitution	USD 55	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 55	In-stock	Estimated Time of Arrival: December 31
Solid
500 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
1 g	USD 80	In-stock	Estimated Time of Arrival: December 31
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Based on 4 publication(s) in Google Scholar

Other Forms of Primaquine diphosphate:

Primaquine-d₃ diphosphate Get quote
Primaquine Get quote
Primaquine diphosphate (Standard) Get quote

4 Publications Citing Use of MCE Primaquine diphosphate

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Biological Activity
Purity & Documentation
References
Customer Review

Description

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

IC₅₀ & Target

Plasmodium

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	5 μM Compound: PQ diphosphate	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
CAPAN-1	IC₅₀	14.24 μM Compound: PQ diphosphate	Cytotoxicity against human Capan1 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human Capan1 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
HCT-116	IC₅₀	13.99 μM Compound: PQ	Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells measured after 72 hrs by MTT assay	[PMID: 31431364]
HCT-116	IC₅₀	44.22 μM Compound: PQ diphosphate	Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
HEK293	IC₅₀	10.96 μM Compound: PQ	Antiproliferative activity against human HEK293 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HEK293 cells measured after 72 hrs by MTT assay	[PMID: 31431364]
HL-60	IC₅₀	11.36 μM Compound: PQ diphosphate	Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HL60 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
K562	IC₅₀	12.04 μM Compound: PQ diphosphate	Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human K562 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
L6	IC₅₀	27.1 μg/mL Compound: PQ diphsophate	Cytotoxicity against rat L6 cells after 70 hrs by Alamar Blue-based assay Cytotoxicity against rat L6 cells after 70 hrs by Alamar Blue-based assay	[PMID: 29220797]
L6	IC₅₀	59.5 μM Compound: PQ diphosphate	Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 70 hrs by Alamar blue assay Cytotoxicity against rat L6 cells assessed as reduction in cell viability after 70 hrs by Alamar blue assay	[PMID: 29407988]
MCF7	IC₅₀	5 μM Compound: PQ diphosphate	Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
MCF7	IC₅₀	8.73 μM Compound: PQ	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 31431364]
NCI-H460	IC₅₀	10 μM Compound: PQ diphosphate	Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]
NCI-H460	IC₅₀	19.84 μM Compound: PQ	Antiproliferative activity against human H460 cells measured after 72 hrs by MTT assay Antiproliferative activity against human H460 cells measured after 72 hrs by MTT assay	[PMID: 31431364]
SW-620	IC₅₀	14 μM Compound: PQ diphosphate	Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against human SW620 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 29407988]

In Vitro

Primaquine diphosphate 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 diphosphate 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 hours
Result:	Decreases breast cancer cell viability.

In Vivo

Primaquine (5-25 mg/kg; p.o; daily; for 3 days) diphosphate 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

455.34

Formula

C₁₅H₂₇N₃O₉P₂

CAS No.

63-45-6

Appearance

Solid

Color

Red brown to orange

SMILES

CC(NC1=C2N=CC=CC2=CC(OC)=C1)CCCN.O=P(O)(O)O.O=P(O)(O)O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 250 mg/mL (549.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (54.90 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1962 mL	10.9808 mL	21.9616 mL
5 mM	0.4392 mL	2.1962 mL	4.3923 mL
10 mM	0.2196 mL	1.0981 mL	2.1962 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 50 mg/mL (109.81 mM); Clear solution; Need ultrasonic

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.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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).

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (278 KB) SDS (584 KB)

COA (252 KB) HNMR (229 KB) LCMS (266 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

H₂O / DMSO	1 mM	2.1962 mL	10.9808 mL	21.9616 mL	54.9040 mL
	5 mM	0.4392 mL	2.1962 mL	4.3923 mL	10.9808 mL
	10 mM	0.2196 mL	1.0981 mL	2.1962 mL	5.4904 mL
	15 mM	0.1464 mL	0.7321 mL	1.4641 mL	3.6603 mL
	20 mM	0.1098 mL	0.5490 mL	1.0981 mL	2.7452 mL
	25 mM	0.0878 mL	0.4392 mL	0.8785 mL	2.1962 mL
	30 mM	0.0732 mL	0.3660 mL	0.7321 mL	1.8301 mL
	40 mM	0.0549 mL	0.2745 mL	0.5490 mL	1.3726 mL
	50 mM	0.0439 mL	0.2196 mL	0.4392 mL	1.0981 mL
DMSO	60 mM	0.0366 mL	0.1830 mL	0.3660 mL	0.9151 mL
	80 mM	0.0275 mL	0.1373 mL	0.2745 mL	0.6863 mL
	100 mM	0.0220 mL	0.1098 mL	0.2196 mL	0.5490 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Primaquine diphosphate 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:

Primaquine diphosphate63-45-6PrimaquinePrimaquine bisphosphateParasiteparasiticmalarialatehepaticstageslatenttissueInhibitorinhibitorinhibit

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Primaquine diphosphate (Synonyms: Primaquine phosphate; Primaquine bisphosphate)

Customer Review

Other Forms of Primaquine diphosphate:

Primaquine diphosphate Related Antibodies

4 Publications Citing Use of MCE Primaquine diphosphate

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Parasite Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Primaquine diphosphate Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Primaquine diphosphate Related Classifications

Keywords:

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