Chlorpromazine hydrochloride 是一种口服有效的、可透过血脑屏障的抗精神病剂,能有效拮抗D2多巴胺受体和5-HT2A,已广泛用于精神分裂症和其他精神疾病。Chlorpromazine hydrochloride 可通过多种途径发挥抗癌活性,包括抗增殖、诱导自噬和周期停滞 (G2-M 期)、抑制细胞色素 c 氧化酶 (CcO)、抑制肿瘤生长和转移以及抑制肿瘤免疫逃逸等。Chlorpromazine hydrochloride 还能阻断 hNav1.7 通道 (IC50=25.9 μM; 浓度依赖的方式) 和 HERG 钾通道 (IC50=21.6 μM) ,其在止痛以及心律失常方面也具有较好的研究潜力。Chlorpromazine hydrochloride 也能抑制网格蛋白介导的内吞作用。
生物活性 | Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonisesD2 dopamine receptorsand5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction ofautophagyand cycle arrest (G2-M phase), inhibition ofcytochrome c oxidase(CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis[1][2][3][4][5]. |
IC50& Target | D2 dopamine receptors; 5-HT2A[1][6]. |
体外研究 (In Vitro) | Chlorpromazine hydrochloride (0, 10, 20, 40 μM; 0, 24, 48 h) inhibits growth of U-87MG glioma cells in a dose- and time- dependent manner[2]. Chlorpromazine hydrochloride (20 μM; 0, 12, 24, 48 h) decreases the levels of cyclin A and cyclin B1 in U-87MG glioma cells, 12 h later[2]. Chlorpromazine hydrochloride (20 μM) causes inhibition of cell cycle progression[2]. Chlorpromazine hydrochloride (10 μM; 1 h) significantly suppresses the sEV internalization and dramatically reduces MDSCs in sEV-treated bone marrow cells (MDSCs can significantly suppress the immune cell response, causing immunosuppression in cancer cells)[3]. Chlorpromazine hydrochloride (3, 10, 20, 40, 60 μM) blocks the hNav1.7 current in a concentration-dependent manner[4]. Chlorpromazine hydrochloride blocks HERG potassium channels with an IC50value of 21.6 μM and a Hill coefficient of 1.11[5].
Cell Proliferation Assay[2] Cell Line: | U-87MG glioma cells | Concentration: | 0, 10, 20, 40 μM | Incubation Time: | 0, 24, 48 h | Result: | Showed anti-proliferative activity in a dose- and time-dependent manner. |
Immunofluorescence[3] Cell Line: | Bone marrow cells (sEV-treated) | Concentration: | 10 μM | Incubation Time: | 1 h | Result: | Reduced MDSCs and suppressed the sEV internalization. |
Western Blot Analysis[2] Cell Line: | U-87MG glioma cells | Concentration: | 20 μM | Incubation Time: | 0, 12, 24, 48 h | Result: | Decreased the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged. |
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体内研究 (In Vivo) | Chlorpromazine hydrochloride (20 mg/kg; i.p.; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2].
Animal Model: | 5- to 6-week-old athymic nude mice bearing intracranial U-87MG xenograft tumors[2]. | Dosage: | 20 mg/kg | Administration: | Injected intraperitoneally; single daily for 7 days | Result: | Inhibited tumor growth on day 17. |
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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 and light *该产品在溶液状态不稳定,建议您现用现配,即刻使用。 |
溶解性数据 | In Vitro: H2O : 100 mg/mL(281.43 mM;Need ultrasonic) DMSO : ≥ 60 mg/mL(168.86 mM) *"≥" means soluble, but saturation unknown. 配制储备液 1 mM | 2.8143 mL | 14.0714 mL | 28.1429 mL | 5 mM | 0.5629 mL | 2.8143 mL | 5.6286 mL | 10 mM | 0.2814 mL | 1.4071 mL | 2.8143 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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (7.04 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (7.04 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.85 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.85 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.85 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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