SJPYT-195
Based on 1 Customer Validation
SJPYT-195 is a cytotoxic GSPT1 degrader and can be used for PROTAC synthesis.
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: 98.07%
- CAS 番号: 2973762-16-0
- 分子式: C35H34N6O8
- 分子量:666.68
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
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Cell Line
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Type | Value | Description | References |
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| SNU-C4 | CC50 |
3.3 nM
Compound: 18; SJPYT-195
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Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
Cytotoxicity against PXR knock in human SNU-C4 cells measured after 72 hrs by celltiter-glo assay
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[PMID: 35978691] |
SJPYT-195 (24 h) potently and efficaciously reduces endogenous PXR (pregnane X receptor) protein in the colorectal SNU-C4 cell line (SNU-C4 3xFLAG-PXR KI cells), with a half maximal degradation concentration (DC50) of 310 ± 130 nM and maximum degradation efficacy (DMax) of 85 ± 1%[1].
SJPYT-195 reduces PXR protein through the degradation of GSPT1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2973762-16-0
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性状 Solid
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分子量 666.68
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分子式 C35H34N6O8
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Color White to off-white
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SMILES
O=C(C1=C(C)N(C2=CC(OC)=CC=C2OC)N=N1)NC3=CC(OC4=CC=CC(C(N5C(CC6)C(NC6=O)=O)=O)=C4C5=O)=CC(C(C)(C)C)=C3
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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 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (75.00 mM; ultrasonic and warming and heat to 60°C; 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 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.12 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.67 mg/mL (2.50 mM); Clear solution
This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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 (272 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 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 | 1.5000 mL | 7.4999 mL | 14.9997 mL | 37.4993 mL |
| 5 mM | 0.3000 mL | 1.5000 mL | 2.9999 mL | 7.4999 mL | |
| 10 mM | 0.1500 mL | 0.7500 mL | 1.5000 mL | 3.7499 mL | |
| 15 mM | 0.1000 mL | 0.5000 mL | 1.0000 mL | 2.5000 mL | |
| 20 mM | 0.0750 mL | 0.3750 mL | 0.7500 mL | 1.8750 mL | |
| 25 mM | 0.0600 mL | 0.3000 mL | 0.6000 mL | 1.5000 mL | |
| 30 mM | 0.0500 mL | 0.2500 mL | 0.5000 mL | 1.2500 mL | |
| 40 mM | 0.0375 mL | 0.1875 mL | 0.3750 mL | 0.9375 mL | |
| 50 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7500 mL | |
| 60 mM | 0.0250 mL | 0.1250 mL | 0.2500 mL | 0.6250 mL |