Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT 2A , 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 of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNa v 1.7 channels (IC 50 =25.9 μM; concentration-dependent) and HERG potassium channels (IC 50 =21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.
性状
Solid
IC50 & Target[1][2]
D2 dopamine receptors; 5-HT2A.
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.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.Chlorpromazine hydrochloride (20 μM) causes inhibition of cell cycle progression.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).Chlorpromazine hydrochloride (3, 10, 20, 40, 60 μM) blocks the hNav1.7 current in a concentration-dependent manner.Chlorpromazine hydrochloride blocks HERG potassium channels with an IC50 value of 21.6 μM and a Hill coefficient
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. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: 5- to 6-week-old
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。
参考文献
[1]. Kamgar-Dayhoff P, et al. Multifaceted effect of chlorpromazine in cancer: implications for cancer treatment. Oncotarget. 2021 Jul 6;12(14):1406-1426. [2]. Shin SY, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells. Carcinogenesis. 2013 Sep;34(9):2080-9.
溶解度数据
In Vitro: H2O : 100 mg/mL (281.43 mM; Need ultrasonic)DMSO : ≥ 60 mg/mL (168.86 mM)