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Pyronaridine Tetraphosphate

Catalog No.
A1931
Antimalarial agent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$50.00
In stock
Evaluation Sample
$28.00
In stock
100mg
$70.00
In stock
250mg
$150.00
In stock

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Email: [email protected]

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Background

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.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at RT
M.Wt910.03
Cas No.76748-86-2
FormulaC29H32ClN5O24H3PO4
SynonymsMalaridine
Solubility≥12.25mg/mL in DMSO with gentle warming
Chemical Name4-[(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
SDFDownload SDF
Canonical SMILESCOC1=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
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

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.

Biological Activity

Description Pyronaridine Tetraphosphate is a common antimalarial agent.
Targets MDR multidrug resistance          
IC50            

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