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Pyronaridine Tetraphosphate (Synonyms: PND)

Catalog No.GC17403

An antimalarial agent

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Pyronaridine Tetraphosphate Chemical Structure

Cas No.: 76748-86-2

Taille Prix Stock Qté
10mM (in 1mL DMSO)
36,00 $US
En stock
100mg
54,00 $US
En stock
250mg
116,00 $US
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Sample solution is provided at 25 µL, 10mM.

Description of Pyronaridine Tetraphosphate

Pyronaridine (PND), a synthetic quinolone derivative frequently prescribed for the treatment of malaria, is a selective and potent multidrug resistance (MDR) modulator of Pgp-mediated MDR that inhibits the proliferation of a variety of tumor cells, including myeloid leukemia (K562 and K562/A02), epidermoid carcinoma (KB and KBV200), breast carcinoma (MCF-7 and MCF-7/ADR), ovarian carcinoma (SKOV3, ES-2 and PA-1), gastric carcinoma (BGC-823), colon carcinoma (LoVo), hepatocellular carcinoma (SMMZ-7721 and QGY-7703), with the half maximal inhibition concentration IC50 values of 8.3 μM, 5.6 μM, 20.8 μM, 14.5 μM, 9.5 μM, 11 μM, 9.7 μM, 12.9 μM, 15.7 μM, 14.9 μM, 21.4 μM, 10.9 μM and 17.1 μM respectively [1].

References:
[1] Qi J, Wang S, Liu G, Peng H, Wang J, Zhu Z, Yang C. Pyronaridine, a novel modulator of P-glycoprotein-mediated multidrug resistance in tumor cells in vitro and in vivo. Biochem Biophys Res Commun. 2004 Jul 9;319(4):1124-31.

Protocol of Pyronaridine Tetraphosphate

Cell experiment [1]:

Cell lines

K562/A02 and MCF-7/ADR cells

Preparation method

The solubility of this compound in DMSO is > 12.25 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0 ~ 4.4 μM; 72 hrs

Applications

Pyronaridine Tetraphosphate significantly enhanced the effect of DOX on K562/A02 and MCF-7/ADR cells, without affecting the effect of DOX on parent K562 and MCF-7 cells. At a concentration of 4.4 μM, Pyronaridine Tetraphosphate resulted in a ~ 295-fold and a 30-fold DOX sensitization in K562/A02 and MCF-7/ADR cells, respectively.

Animal experiment [1]:

Animal models

Nude mice bearing K562 and K562/A02 tumors

Dosage form

40 mg/kg; i.p.; q3d

Applications

Pyronaridine Tetraphosphate in combination with 4 mg/kg DOX exhibited no effect on the antitumor effect of DOX on K562 tumors, but significantly enhanced the antitumor effect of DOX on K562/A02 tumors. When DOX given at sub-MTD doses (1 or 2 mg/kg), the addition of Pyronaridine Tetraphosphate dose-dependently inhibited the growth of K562 tumors, but showed the minimal effect on K562/A02 tumors.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Qi J, Wang S, Liu G, Peng H, Wang J, Zhu Z, Yang C. Pyronaridine, a novel modulator of P-glycoprotein-mediated multidrug resistance in tumor cells in vitro and in vivo. Biochem Biophys Res Commun. 2004 Jul 9;319(4):1124-31.

Chemical Properties of Pyronaridine Tetraphosphate

Cas No. 76748-86-2 SDF
Synonymes PND
Chemical Name 4-[(7-chloro-2-methoxy-1,5-dihydrobenzo[b][1,5]naphthyridin-10-yl)imino]-2,6-bis(pyrrolidin-1-ylmethyl)cyclohexa-2,5-dien-1-one;phosphoric acid
Canonical SMILES COC1=CC=C2C(=C(C3=C(N2)C=C(C=C3)Cl)N=C4C=C(C(=O)C(=C4)CN5CCCC5)CN6CCCC6)N1.OP(=O)(O)O.OP(=O)(O)O.OP(=O)(O)O.OP(=O)(O)O
Formula C29H32ClN5O24H3PO4 M.Wt 910.03
Solubility ≥ 12.25mg/mL in DMSO with gentle warming Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Pyronaridine Tetraphosphate

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.0989 mL 5.4943 mL 10.9886 mL
5 mM 219.8 μL 1.0989 mL 2.1977 mL
10 mM 109.9 μL 549.4 μL 1.0989 mL
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In vivo Formulation Calculator (Clear solution) of Pyronaridine Tetraphosphate

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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