Chlorpromazine HCl (Synonyms: CPZ) |
| Catalog No.GC14216 |
Chlorpromazine HCl is an orally effective, blood-brain-permeable phenothiazine antipsychotic that can effectively antagonize D2 dopamine receptors and 5-HT2A and has a strong sedative effect.
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Cas No.: 69-09-0
Sample solution is provided at 25 µL, 10mM.
Chlorpromazine HCl is an orally effective, blood-brain-permeable phenothiazine antipsychotic that can effectively antagonize D2 dopamine receptors and 5-HT2A and has a strong sedative effect[1, 2]. Chlorpromazine HCl has anticancer activities, including anti-proliferation, induction of cell autophagy and cell cycle arrest, inhibition of cytochrome c oxidase, inhibition of tumor growth and metastasis, and inhibition of tumor immune escape[3]. Chlorpromazine HCl can block hNav1.7 channels and hERG potassium channels[4, 5].
In vitro, treatment of U-87MG cells with Chlorpromazine HCl (10-40μM) for 24h and 48h reduced cell viability, cell proliferation, and intracellular cyclin A and cyclin B1 levels in a dose- and time-dependent manner[6]. Chlorpromazine HCl (10μM) treatment of mouse bone marrow cells for 1h significantly inhibited the internalization of small extracellular vesicles (sEVs) and significantly reduced the number of myeloid-derived suppressor cells (MDSCs)[7].
In vivo, Chlorpromazine HCl (20mg/kg) was intraperitoneally injected into U-87MG glioma cell xenograft mice for 24 days and significantly inhibited tumor growth, with a tumor growth inhibition rate of 43.5% on day 24[6].
References:
[1] Asano T, Tanaka K, Tada A, et al. Ameliorative effect of chlorpromazine hydrochloride on visceral hypersensitivity in rats: possible involvement of 5‐HT2A receptor[J]. British Journal of Pharmacology, 2017, 174(19): 3370-3381.
[2] Suzuki H, Gen K, Inoue Y. Comparison of the anti-dopamine D2 and anti-serotonin 5-HT2A activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof[J]. Journal of Psychopharmacology, 2013, 27(4): 396-400.
[3] Kamgar-Dayhoff P, Brelidze T I. Multifaceted effect of chlorpromazine in cancer: Implications for cancer treatment[J]. Oncotarget, 2021, 12(14): 1406.
[4] Lee S J, Kim D H, Hahn S J, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1. 7[J]. Neuroscience Letters, 2017, 639: 1-7.
[5] Thomas D, Wu K, Kathöfer S, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels[J]. British journal of pharmacology, 2003, 139(3): 567-574.
[6] Shin S Y, Lee K S, Choi Y K, et al. The antipsychotic agent chlorpromazine induces autophagic cell death by inhibiting the Akt/mTOR pathway in human U-87MG glioma cells[J]. Carcinogenesis, 2013, 34(9): 2080-2089.
[7] Yang Z, Huo Y, Zhou S, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production[J]. Cell Metabolism, 2022, 34(12): 2018-2035. e8.
| Cell experiment [1]: | |
Cell lines | U-87MG cells |
Preparation Method | U-87MG cells (2×103 cells per sample) seeded into 96 well plates were treated with Chlorpromazine HCl at increasing concentrations (0, 10, 20 and 40μM) for different time periods (0, 24 and 48h). Determination of cell viability and cell proliferation. |
Reaction Conditions | 0-40μM; 24, 48h |
Applications | Chlorpromazine HCl decreases cell viability and proliferation in a dose- and time-dependent manner. |
| Animal experiment [1]: | |
Animal models | Athymic nude mice |
Preparation Method | U-87MG glioma cells (1×106 cells in 100μl serum-free DMEM) were inoculated subcutaneously into the right flank of 5- to 6-week-old athymic nude mice. When tumors reached an average volume of ~100mm3, 100μl of PBS (control) or Chlorpromazine HCl (20mg/kg) were injected intraperitoneally daily. Mice were killed on day 24 by exposure to CO2 to compare tumor size of skin xenograft tumors. |
Dosage form | 20mg/kg; i.p. |
Applications | Chlorpromazine HClCPZ treatment significantly inhibited xenograft tumor growth compared with PBS (control) treatment, with a tumor growth inhibition rate of 43.5% on day 24. |
References: | |
| Cas No. | 69-09-0 | SDF | |
| Synonyms | CPZ | ||
| Chemical Name | 3-(2-chlorophenothiazin-10-yl)-N,N-dimethylpropan-1-amine;hydrochloride | ||
| Canonical SMILES | CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl.Cl | ||
| Formula | C17H19ClN2S.HCl | M.Wt | 355.33 |
| Solubility | ≥ 17.8 mg/mL in DMSO, ≥ 74.8 mg/mL in EtOH, ≥ 71.4 mg/mL in Water | Storage | Store at RT,protect from light,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 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 |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >99.50%
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