BSJ-5-63
Based on 1 publication(s) in Google Scholar
BSJ-5-63 is a potent CDK12, CDK7, CDK9 PROTAC degrader. BSJ-5-63 BSJ-5-63 decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K. BSJ-5-63 decreases the mRNA expression of BRCA1, BRCA2. BSJ-5-63 shows anticancer activity and has the potential for the research of prostate cancer.
(Pink: CDK12 and CDK7 and CDK9 ligand (HY-150948); Blue: VHL ligand (HY-112078); Black: linker (HY-W140827)).
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: 99.97%
- CAS 番号: 2519823-37-9
- 分子式: C52H74ClN9O6S2
- 分子量:1020.78
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保管条件:
Store at room temperature 3 years.
In solvent -80°C, 2 years , -20°C, 1 year
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
MedChemExpress（MCE）の使用を引用している文献 BSJ-5-63
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生物活性
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CDK12 |
CDK7 |
CDK9 |
BSJ-5-63 (0-1000 nM; 8 h) decreases the protein expression of CDK12, CDK7, CDK9, RNAPII, Cyclin K in a dose-dependent manner[1].
BSJ-5-63 (0-1000 nM; 8, 16, 24 h) decreases the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP, C4-2B, 22Rv1 cells
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Concentration:62.5, 125, 250, 500, 1000 nM
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Incubation Time:8 h
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Result:Decreased the protein expression of CDK12, CDK7, CDK9, P-RNAPII Ser2, P-RNAPII Ser5, P-RNAPII Ser7, RNAPII, Cyclin K in a dose-dependent manner.
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Cell Line:LNCaP, C4-2B, 22Rv1 cells
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Concentration:62.5, 125, 250, 500, 1000 nM
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Incubation Time:8, 16, 24 h
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Result:Decreased the mRNA expression of BRCA1, BRCA2 in a dose and time dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4-5 weeks, Male ICR-SCID mice (22Rv1 cells)[1]
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Dosage:50 mg/kg
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Administration:I.p.; daily for 12 days
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Result:Significantly inhibited the growth of 22Rv1 tumors and tumor weight was significantly reduced and increased in the number of apoptotic cells, daily administration resulted in approximately 10% weight loss in mice.
化学情報
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CAS 番号 2519823-37-9
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性状 Solid
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分子量 1020.78
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分子式 C52H74ClN9O6S2
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Color White to off-white
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SMILES
O=S(C1=CC=CC=C1NC2=NC(N[C@H]3CN(CCCCCCCCCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)CCC3)=NC=C2Cl)(C(C)C)=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
Store at room temperature 3 years
In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2025 Nov 21:2025.11.20.689563. PMID: 41332615
溶剤 & 溶解度
DMSO : 100 mg/mL (97.96 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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.
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 (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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9796 mL | 4.8982 mL | 9.7964 mL | 24.4911 mL |
| 5 mM | 0.1959 mL | 0.9796 mL | 1.9593 mL | 4.8982 mL | |
| 10 mM | 0.0980 mL | 0.4898 mL | 0.9796 mL | 2.4491 mL | |
| 15 mM | 0.0653 mL | 0.3265 mL | 0.6531 mL | 1.6327 mL | |
| 20 mM | 0.0490 mL | 0.2449 mL | 0.4898 mL | 1.2246 mL | |
| 25 mM | 0.0392 mL | 0.1959 mL | 0.3919 mL | 0.9796 mL | |
| 30 mM | 0.0327 mL | 0.1633 mL | 0.3265 mL | 0.8164 mL | |
| 40 mM | 0.0245 mL | 0.1225 mL | 0.2449 mL | 0.6123 mL | |
| 50 mM | 0.0196 mL | 0.0980 mL | 0.1959 mL | 0.4898 mL | |
| 60 mM | 0.0163 mL | 0.0816 mL | 0.1633 mL | 0.4082 mL | |
| 80 mM | 0.0122 mL | 0.0612 mL | 0.1225 mL | 0.3061 mL |
BSJ-5-63 関連分類
HY-162706 関連分類
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