CSRM617 (hydrochloride)
Based on 1 publication(s) in Google Scholar
CSRM617 hydrochloride is a selective small-molecule inhibitor of the transcription factor ONECUT2 (OC2, a master regulator of androgen receptor) with a Kd of 7.43 uM in SPR assays, binding to OC2-HOX domain directly. CSRM617 hydrochloride induces apoptosis by appearance of cleaved Caspase-3 and PARP. CSRM617 hydrochloride is well tolerated in the prostate cancer mouse model
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- 純度 : 99.97%
- CAS 番号: 1353749-74-2
- 分子式: C10H14ClN3O5
- 分子量:291.69
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 CSRM617 hydrochloride
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生物活性
製品説明
体外実験
CSRM617 (0.01-100 μM; 48 hours) hydrochloride inhibits cell growth in several PC cell lines: PC-3, 22RV1, LNCaP, C4-2 cells[1]. CSRM617 (10-20 μM; 48 hours) hydrochloride induces apoptosis in 22Rv1 cells results in cell death in a concentration-dependent fashion[1]. CSRM617 (20 μM; 72 hours) hydrochloride induces apoptosis in 22Rv1 cells by appearance of cleaved Caspase-3 and PARP[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice with 22Rv1 xenograft[1]
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Dosage:50 mg/kg
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Administration:Oral administration; daily, for 20 days
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Result:Elicited a significant reduction in the onset and growth of diffuse metastases.
化学情報
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CAS 番号 1353749-74-2
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性状 Solid
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分子量 291.69
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分子式 C10H14ClN3O5
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Color White to off-white
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SMILES
O=C(C(CO)N)N/N=C/C1=CC=C(C(O)=C1O)O.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Cancers (Basel)
Tumor-Associated Fibroblast-Derived Exosomal circDennd1b Promotes Pituitary Adenoma Progression by Modulating the miR-145-5p/ONECUT2 Axis and Activating the MAPK Pathway. [Abstract]2023 Jun 27;15(13):3375. PMID: 37444485
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (342.83 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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)
体内:
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 (8.57 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.57 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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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 (sealed storage, away from moisture). 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 | 3.4283 mL | 17.1415 mL | 34.2830 mL | 85.7074 mL |
| 5 mM | 0.6857 mL | 3.4283 mL | 6.8566 mL | 17.1415 mL | |
| 10 mM | 0.3428 mL | 1.7141 mL | 3.4283 mL | 8.5707 mL | |
| 15 mM | 0.2286 mL | 1.1428 mL | 2.2855 mL | 5.7138 mL | |
| 20 mM | 0.1714 mL | 0.8571 mL | 1.7141 mL | 4.2854 mL | |
| 25 mM | 0.1371 mL | 0.6857 mL | 1.3713 mL | 3.4283 mL | |
| 30 mM | 0.1143 mL | 0.5714 mL | 1.1428 mL | 2.8569 mL | |
| 40 mM | 0.0857 mL | 0.4285 mL | 0.8571 mL | 2.1427 mL | |
| 50 mM | 0.0686 mL | 0.3428 mL | 0.6857 mL | 1.7141 mL | |
| 60 mM | 0.0571 mL | 0.2857 mL | 0.5714 mL | 1.4285 mL | |
| 80 mM | 0.0429 mL | 0.2143 mL | 0.4285 mL | 1.0713 mL | |
| 100 mM | 0.0343 mL | 0.1714 mL | 0.3428 mL | 0.8571 mL |
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