Pyronaridine Tetraphosphate
(Synonyms: 4-[(7-氯-2-甲氧基-1,5-二氢吡啶并[3,2-b]喹啉-10-基)亚氨]-2,6-二(吡咯烷-1-基甲基)环己-2,5-二烯-1-酮磷酸盐(1:4),Malaridine) 目录号 : GC17403
An antimalarial agent
Cas No.:76748-86-2
Sample solution is provided at 25 µL, 10mM.
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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.
| 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. | |
| Cas No. | 76748-86-2 | SDF | |
| 别名 | 4-[(7-氯-2-甲氧基-1,5-二氢吡啶并[3,2-b]喹啉-10-基)亚氨]-2,6-二(吡咯烷-1-基甲基)环己-2,5-二烯-1-酮磷酸盐(1:4),Malaridine | ||
| 化学名 | 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 | ||
| 分子式 | C29H32ClN5O24H3PO4 | 分子量 | 910.03 |
| 溶解度 | ≥ 12.25mg/mL in DMSO with gentle warming | 储存条件 | Store at RT |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.0989 mL | 5.4943 mL | 10.9886 mL |
| 5 mM | 0.2198 mL | 1.0989 mL | 2.1977 mL |
| 10 mM | 0.1099 mL | 0.5494 mL | 1.0989 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet