PS121912
Based on 1 Customer Validation
PS121912 is a selective vitamin D receptor (VDR)-coregulator inhibitor. PS121912 has acceptable metabolic stability in vivo. PS121912 can be used for the research of cancer.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 96.40%
- CAS 番号: 1529814-60-5
- 分子式: C24H21F3N2O
- 分子量:410.43
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Anti-Cancer Compound Library
HY-L025
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Transcription Factor-Targeted Library
HY-L090
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Nuclear Receptor Compound Library
HY-L126
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Osteogenesis Compound Library
HY-L131
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Highly Selective Inhibitors Library
HY-L158
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Cell Death Library
HY-L162
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
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High-Throughput Bioactive Compound Library
HY-L205
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
0.59 μM
Compound: PS121912
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Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay
Inhibition of 1,25(OH)2D3-induced VDR (unknown origin)-mediated CYP24A1 transcription expressed in HEK293T cells after 16 hrs by luciferase reporter gene assay
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[PMID: 24799995] |
| HEK-293T | IC50 |
8.1 μM
Compound: PS121912
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Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay
Inhibition of 1,25(OH)2D3-induced VDR-LBD (unknown origin)-mediated GAL4-labeled SRC1 transcription expressed in HEK293T cells after 16 hrs by two-hydrid luciferase reporter gene assay
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[PMID: 24799995] |
| HL-60 | EC50 |
20 μM
Compound: PS121912
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Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay
Cytotoxicity against human HL60 cells assessed as ATP level after 18 hrs by CellTiter-Glo assay
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[PMID: 24799995] |
| HL-60 | EC50 |
20 μM
Compound: PS121912
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Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay
Cytotoxicity against human HL60 cells assessed as cell viability after 18 hrs by CellTiter-Fluor assay
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[PMID: 24799995] |
PS121912 behaves like a VDR antagonist at low concentrations but interacts with more targets at higher concentrations leading to apoptosis mediated by caspase 3/7 activation[1].
PS121912 (combined with 1,25-(OH)2D3)reduces the transcription levels of cyclin A and D thus arresting HL-60 cells in the S or G2/M phase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cancer cells consisting of DU145 (prostate), Caco2 (colon), HL-60 (monocytes), and SKOV3 (ovary)
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Concentration:0-100 μM
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Incubation Time:18 h
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Result:Induced apoptosis in all four cancer cells, with HL-60 cells being the most sensitive.
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Cell Line:Four different cancer cell lines (DU145 prostate cancer, Caco2 colon cancer, SKOV3 ovarian cancer and HL-60 monocytes)
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Concentration:0.5, 2 μM
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Incubation Time:5 days
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Result:Amplified the growth inhibition of cancer cells caused by 1.25-(OH)2Ds without being antiproliferative by itself at sub-micromolar concentrations.
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Cell Line:HL-60 cells
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Concentration:500 nM
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Incubation Time:18 h
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Result:Reduced expression of HSP60 and Survivin and elevated the levels of pro-apoptotic BIM.
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Cell Line:HL-60 cells
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Concentration:3 μM
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Incubation Time:18 h
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Result:Induced the expression of caspase 3 and caspase 7 mRNA levels.
化学情報
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CAS 番号 1529814-60-5
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性状 Solid
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分子量 410.43
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分子式 C24H21F3N2O
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Color Off-white to light yellow
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SMILES
FC(C1=CC=C(NC(C2=CC=C(OC)C=C2)C3=C(C)NC4=C3C=CC=C4)C=C1)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (243.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4365 mL | 12.1823 mL | 24.3647 mL | 60.9117 mL |
| 5 mM | 0.4873 mL | 2.4365 mL | 4.8729 mL | 12.1823 mL | |
| 10 mM | 0.2436 mL | 1.2182 mL | 2.4365 mL | 6.0912 mL | |
| 15 mM | 0.1624 mL | 0.8122 mL | 1.6243 mL | 4.0608 mL | |
| 20 mM | 0.1218 mL | 0.6091 mL | 1.2182 mL | 3.0456 mL | |
| 25 mM | 0.0975 mL | 0.4873 mL | 0.9746 mL | 2.4365 mL | |
| 30 mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 2.0304 mL | |
| 40 mM | 0.0609 mL | 0.3046 mL | 0.6091 mL | 1.5228 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4873 mL | 1.2182 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4061 mL | 1.0152 mL | |
| 80 mM | 0.0305 mL | 0.1523 mL | 0.3046 mL | 0.7614 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6091 mL |
PS121912 関連分類
HY-103053 関連分類
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