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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.
| Physical Appearance | A solid |
| Storage | Store at RT |
| M.Wt | 910.03 |
| Cas No. | 76748-86-2 |
| Formula | C29H32ClN5O24H3PO4 |
| Synonyms | Malaridine |
| Solubility | insoluble in EtOH; ≥12.25 mg/mL in DMSO with gentle warming; ≥8.7 mg/mL in H2O |
| 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 |
| SDF | Download SDF |
| 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 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment [1]: | |
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Cell lines |
K562/A02 and MCF-7/ADR cells |
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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. |
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Reacting condition |
0 ~ 4.4 μM; 72 hrs |
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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]: | |
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Animal models |
Nude mice bearing K562 and K562/A02 tumors |
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Dosage form |
40 mg/kg; i.p.; q3d |
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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. |
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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. |
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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. |
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| Description | Pyronaridine Tetraphosphate is a common antimalarial agent. | |||||
| Targets | MDR multidrug resistance | |||||
| IC50 | ||||||
Quality Control & MSDS
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Chemical structure
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