Quinacrine (Mepacrine) dihydrochloride 是一种有效的，具有口服活性的抗疟剂 (antimalarial)，在体内外均具有抗肿瘤作用。Quinacrine dihydrochloride 抑制 NF-κB 并激活 p53 信号转导，诱导肿瘤细胞发生凋亡 (apoptosis)。
| 生物活性 | Quinacrine (Mepacrine) dihydrochloride is an orally bioavailableantimalarialagent, which possess anticancer effect both in vitro and vivo. Quinacrine dihydrochloride suppressesNF-κBand activate p53 signaling, which results in the induction of theapoptosis[1]. |
体外研究
(In Vitro) | Quinacrine (5-20 μM; 24 hours) inhibits the growth of SGC-7901 cells[1].
Quinacrine (7.5 and 15 μM; 24 hours) induces apoptosis in SGC-7901 cells, which is associated with mitochondria-dependent signal pathway and involves p53 upregulation and caspase-3 activation pathway[1].
Quinacrine (15 μM; 24 hours) treatment significantly increased the levels of proapoptotic proteins, including cytochrome c, Bax, and p53, and decreased the levels of antiapoptotic protein Bcl-2, thus shifting the ratio of Bax/Bcl-2 in favor of apoptosis[1].
Cell Viability Assay[1] | Cell Line: | SGC-7901 cells | | Concentration: | 0, 5, 10, 15, and 20 μM | | Incubation Time: | 24 hours | | Result: | Cell viability was inhibited in a dose-dependent manner, and the mean IC50value is 16.18 μM. |
Apoptosis Analysis[1] | Cell Line: | SGC-7901 cells | | Concentration: | 7.5 and 15 μM | | Incubation Time: | 24 hours | | Result: | The percentage of apoptotic cells, including the early phase and late phase apoptosis, increased to 26.30%, compared with control group of 3.37%. |
Western Blot Analysis[1] | Cell Line: | SGC-7901 cells | | Concentration: | 15 μM | | Incubation Time: | 24 hours | | Result: | The relative quantity of cytochrome c protein was upregulated, increased from 0.10 to 0.24.
The relative quantity of p53 protein was dramatically increased, from 0.06 to 0.19.
The Bax/Bcl-2 ratio was dramatically elevated from 1.21 to 2.59. |
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体内研究
(In Vivo) | Quinacrine (100 mg/kg three times per week for two consecutive weeks) significantly suppresses circulating blast cells at days 30/31 and increases the median survival time (MST). Quinacrine does not decrease the body weight of treated animals at the tested dose[2].
| Animal Model: | Female SCID mice with acute myeloid leukemia (AML)-PS model[2] | | Dosage: | 100 mg/kg | | Administration: | Administered by oral gavage (po); three times a week for two consecutive weeks | | Result: | In the first AML mouse in vivo study, evaluation of circulating leukemic cells detected in blood samples (in percent of white blood cells (WBC)) at day 30/31 showed 72% human tumor cells in the control mice, whereas in mice treated with Quinacrine, this was only 2.2%.
The MST of control mice was 34 days whereas it was 46 days in Quinacrine-treated mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : ≥ 44 mg/mL(93.05 mM) H2O : 13.89 mg/mL(29.37 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.1147 mL | 10.5735 mL | 21.1470 mL | | 5 mM | 0.4229 mL | 2.1147 mL | 4.2294 mL | | 10 mM | 0.2115 mL | 1.0574 mL | 2.1147 mL |
*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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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