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Pyronaridine Tetraphosphate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Pyronaridine Tetraphosphate图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
100mg电议
250mg电议

产品介绍
Pyronaridine tetraphosphate 是一种具有口服活性的曼尼希碱抗疟疾剂。

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 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 ℃ 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 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.

产品描述

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.