SJ995973
Based on 1 Customer Validation
SJ995973 is a BRD4 PROTAC degrader with DC50 values of 0.87 nM (12 h) and 0.16 nM (24 h), respectively. SJ995973 induces the formation of a ternary complex between purified BRD4 and CRBN-DDB1 proteins, with an IC50 of 17 nM against CRBN. SJ995973 inhibits the viability of human acute myeloid leukemia cells. SJ995973 can be used in studies related to acute myeloid leukemia and medulloblastoma.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-163169); Black: linker (HY-W004710)).
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: 98.88%
- CAS 番号: 2882065-25-8
- 分子式: C37H40ClN7O5S
- 分子量:730.28
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保管条件:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
PROTACs アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
[1]|
BRD4 0.16 nM (DC50) |
Cereblon 17 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | IC50 |
1.83 nM
Compound: SJ995973; 26
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Cytotoxicity against human MV4-11 cells
Cytotoxicity against human MV4-11 cells
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[PMID: 36202064] |
| MV4-11 | IC50 |
3 pM
Compound: 4c/SJ995973
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Antiproliferative activity against human MV4-11 after 3 days by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 after 3 days by CellTiter-Glo assay
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[PMID: 36274273] |
| MV4-11 | IC50 |
3 pM
Compound: SJ995973; 26
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Cytotoxicity against human MV4-11 cells measured after 96 hrs
Cytotoxicity against human MV4-11 cells measured after 96 hrs
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[PMID: 36202064] |
| MV4-11 | IC50 |
3 pM
Compound: SJ995973
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Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay
Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 3 days by CellTiter-Glo assay
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[PMID: 37178483] |
体外実験
SJ995973 (range of concentrations; 72 h) potently inhibits the viability of MV4-11 cells with an IC50 of 0.003 nM and HD-MB03 cells with an IC50 of 1.83 nM after 3 days of treatment[1].
SJ995973 (0.1 μM, range of concentrations; 4 h, 12 h, 24 h, 48 h) potently and sustainably degrades BRD4 in MV4-11 cells, with a DC50 of 0.87 nM after 12 h and 0.16 nM after 24 h, and achieves >90% depletion of BRD2 and BRD4 within 4 h at 0.1 μM[1].
SJ995973 (0.1 μM, range of concentrations; 12 h, up to 96 h) potently degrades BRD4 in HD-MB03 cells, with a DC50 of 24 nM after 12 h, and sustains BRD4 depletion for 96 h at 0.1 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human acute myeloid leukemia MV4-11 cells
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Concentration:0.01, 1, 100 and 10000 nM
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Incubation Time:0, 4, 8, 12, 24, 32, 48 h
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Result:Achieved > 90% depletion of BRD2 and BRD4 proteins after 4 h at 0.1 μM, with sustained BRD4 depletion for 48 h.
Displayed a BRD4 half-maximum degradation concentration (DC50) of 0.87 nM after 12 h, and a DC50 of 0.16 nM after 24 h, with a maximum degradation (Dmax) of 99%.
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Cell Line:human medulloblastoma HD-MB03 cells
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Concentration:0.1, 1, 10, 100, 1000 nM
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Incubation Time:0, 4, 8, 12, 24, 32, 48, 72 and 92 h
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Result:Achieved sustained BRD4 depletion for the full 96 h incubation at 0.1 μM.
Displayed a BRD4 DC50 of 24 nM after 12 h.
体内実験
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 2882065-25-8
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性状 Solid
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分子量 730.28
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分子式 C37H40ClN7O5S
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Color Off-white to light yellow
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N12)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCCCCNC(COC5=CC=C(C=C5)C6CCC(NC6=O)=O)=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
溶剤 & 溶解度
体外:
DMSO : 100 mg/mL (136.93 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 and light). 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 and light). 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 (3.42 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.
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 and light)
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 (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Min J, et al. Phenyl-Glutarimides: Alternative Cereblon Binders for the Design of PROTACs. Angewandte Chemie (International ed. in English). 2021 Dec 13;60(51):26663-26670. [Content Brief]
[2]. Actis M, et al. Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs. Journal of medicinal chemistry. 2025 Feb 13;68(3):3591-3611. [Content Brief]
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 and light). 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 | 1.3693 mL | 6.8467 mL | 13.6934 mL | 34.2334 mL |
| 5 mM | 0.2739 mL | 1.3693 mL | 2.7387 mL | 6.8467 mL | |
| 10 mM | 0.1369 mL | 0.6847 mL | 1.3693 mL | 3.4233 mL | |
| 15 mM | 0.0913 mL | 0.4564 mL | 0.9129 mL | 2.2822 mL | |
| 20 mM | 0.0685 mL | 0.3423 mL | 0.6847 mL | 1.7117 mL | |
| 25 mM | 0.0548 mL | 0.2739 mL | 0.5477 mL | 1.3693 mL | |
| 30 mM | 0.0456 mL | 0.2282 mL | 0.4564 mL | 1.1411 mL | |
| 40 mM | 0.0342 mL | 0.1712 mL | 0.3423 mL | 0.8558 mL | |
| 50 mM | 0.0274 mL | 0.1369 mL | 0.2739 mL | 0.6847 mL | |
| 60 mM | 0.0228 mL | 0.1141 mL | 0.2282 mL | 0.5706 mL | |
| 80 mM | 0.0171 mL | 0.0856 mL | 0.1712 mL | 0.4279 mL | |
| 100 mM | 0.0137 mL | 0.0685 mL | 0.1369 mL | 0.3423 mL |
SJ995973 関連分類
HY-145125 関連分類
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