| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
D2 dopamine receptors; 5-HT2A[1][6].
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|---|---|
| ln Vitro |
Chlorpromazine hlorpromazine (0, 10, 20, 40 μM; 0, 24, 48 h) suppresses U-87MG glioma cell proliferation in a time- and dose-dependent manner[2]. The levels of cyclin A and cyclin B1 in U-87MG glioma cells are decreased by chlorpromazine (20 μM; 0, 12, 24, 48 h) 12 hours later[2]. Cell cycle progression is inhibited by 20 μM of chlorpromazine[2]. In sEV-treated bone marrow cells, chlorpromazine (10 μM; 1 h) greatly lowers MDSCs and significantly suppresses the internalization of sEV (MDSCs can significantly suppress the immune cell response, producing immunosuppression in cancer cells)[3]. The hNav1.7 current is blocked by chlorpromazine (3, 10, 20, 40, and 60 µM) in a concentration-dependent way[4]. HERG potassium channels are blocked by chlorpromazine, which has an IC50 value of 21.6 µM and a Hill coefficient of 1.11[5].
|
| ln Vivo |
Chlorpromazine (20 mg/kg; ip; single daily for 7 days) inhibits xenograft tumor growth in nude mouse[2].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: U-87MG glioma cells Tested Concentrations: 0, 10, 20, 40 μM Incubation Duration: 0, 24, 48 h Experimental Results: demonstrated anti-proliferative activity in a dose - and time-dependent manner. Immunofluorescence[3] Cell Types: Bone marrow cells (sEV-treated) Tested Concentrations: 10 µM Incubation Duration: 1 h Experimental Results: decreased MDSCs and suppressed the sEV internalization. Western Blot Analysis[2] Cell Types: U-87MG glioma cells Tested Concentrations: 20 μM Incubation Duration: 0, 12, 24, 48 h Experimental Results: diminished the levels of cyclin A and cyclin B1 12 h later, whereas levels of cyclin D1, proliferating cell nuclear antigen and GAPDH remained unchanged. |
| Animal Protocol |
Animal/Disease Models: 5- to 6 weeks old athymic nude mice bearing intracranial U-87MG xenograft tumors[2].
Doses: 20 mg/kg Route of Administration: Injected intraperitoneally (ip); single daily for 7 days Experimental Results: Inhibited tumor growth on day 17. |
| References |
[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. [3]. Yang Z, et al. Cancer cell-intrinsic XBP1 drives immunosuppressive reprogramming of intratumoral myeloid cells by promoting cholesterol production. Cell Metab. 2022 Nov 2:S1550-4131(22)00461-2. [4]. Lee SJ, et al. Mechanism of inhibition by chlorpromazine of the human pain threshold sodium channel, Nav1.7. Neurosci Lett. 2017 Feb 3;639:1-7. [5]. Thomas D, et al. The antipsychotic drug chlorpromazine inhibits HERG potassium channels. Br J Pharmacol. 2003 Jun;139(3):567-74. [6]. Suzuki H, et al. Comparison of the anti-dopamine D₂ and anti-serotonin 5-HT(2A) activities of chlorpromazine, bromperidol, haloperidol and second-generation antipsychotics parent compounds and metabolites thereof. J Psychopharmacol. 2013 Apr;27(4):396-400. |
| Molecular Formula |
C17H19CLN2S
|
|---|---|
| Molecular Weight |
318.86
|
| CAS # |
50-53-3
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| Related CAS # |
Chlorpromazine hydrochloride;69-09-0;Chlorpromazine-d6 hydrochloride;1228182-46-4;Chlorpromazine-d6 oxalate;1276197-23-9
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| SMILES |
CN(C)CCCN1C2=CC=CC=C2SC3=C1C=C(C=C3)Cl
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (313.62 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (7.84 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.84 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1362 mL | 15.6809 mL | 31.3617 mL | |
| 5 mM | 0.6272 mL | 3.1362 mL | 6.2723 mL | |
| 10 mM | 0.3136 mL | 1.5681 mL | 3.1362 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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