TD-428
Based on 1 Customer Validation
TD-428 is a BRD4/BET PROTAC degrader. TD-428 induces the degradation of BRD4 and BET proteins via the ubiquitin-proteasome pathway by recruiting cereblon, thereby inhibiting C-MYC transcription and cancer cell proliferation. TD-428 can be used in the research of metastatic castration-resistant prostate cancer and prostate cancer.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-114406); Black: linker).
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: 98.81%
- CAS 番号: 2334525-50-5
- 分子式: C43H43ClN10O7S
- 分子量:879.38
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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
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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生物活性
製品説明
IC50 & Target
[2]|
BRD4 0.32 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 22Rv1 | DC50 |
0.32 nM
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Half-maximal BRD4 degradation in human 22Rv1 cells.
Half-maximal BRD4 degradation in human 22Rv1 cells.
|
36235052 |
| 22Rv1 | CC50 |
20.1 nM
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Cell proliferation inhibition in human 22Rv1 prostate cancer cells measured via relative cell growth using CelTiter-Glo reagent after 72 h incubation.
Cell proliferation inhibition in human 22Rv1 prostate cancer cells measured via relative cell growth using CelTiter-Glo reagent after 72 h incubation.
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j.ejmech.2019.01.023. |
体外実験
TD-428 (0.1-1000 nM; 24 h) potently degrades BRD4 in 22Rv1 prostate cancer cells, with a DC50 of 0.32 nM[2].
TD-428 (72 h) inhibits the proliferation of 22Rv1 prostate cancer cells with a CC50 of 20.1 nM[2].
TD-428 (10-1000 nM) reduces C-MYC protein levels in 22Rv1 prostate cancer cells[2].
TD-428-mediated degradation of BRD4 in 22Rv1 prostate cancer cells depends on the ubiquitin-proteasome system and Cullin-RING ligase activity[2].
TD-428 (12 h) requires cereblon (CRBN) to induce BRD4 degradation in 22Rv1 prostate cancer cells[2].
TD-428-mediated degradation of BRD4 in 22Rv1 prostate cancer cells is inhibited by excess TD-106 (HY-114406) or JQ1 (HY-13030), confirming that its activity requires simultaneous binding to BRD4 and CRBN[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22Rv1 prostate cancer cells
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Concentration:0.1, 1, 10, 100, 1000 nM
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Incubation Time:24 h
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Result:Induced potent degradation of BRD4 protein with a degradation half-maximal concentration (DC50) of 0.32 nM.
Reduced BRD4 protein levels to 0% of the untreated control at the highest tested concentration (1000 nM).
化学情報
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CAS 番号 2334525-50-5
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性状 Solid
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分子量 879.38
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分子式 C43H43ClN10O7S
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Color Light yellow to green yellow
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SMILES
O=C(NC1=CC(OCCOCCOCCNC2=C3C(N=NN(C(CC4)C(NC4=O)=O)C3=O)=CC=C2)=CC=C1)C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5
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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
体外:
DMSO : 100 mg/mL (113.72 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)
純度とドキュメンテーション
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データシート (282 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 | 1.1372 mL | 5.6858 mL | 11.3716 mL | 28.4291 mL |
| 5 mM | 0.2274 mL | 1.1372 mL | 2.2743 mL | 5.6858 mL | |
| 10 mM | 0.1137 mL | 0.5686 mL | 1.1372 mL | 2.8429 mL | |
| 15 mM | 0.0758 mL | 0.3791 mL | 0.7581 mL | 1.8953 mL | |
| 20 mM | 0.0569 mL | 0.2843 mL | 0.5686 mL | 1.4215 mL | |
| 25 mM | 0.0455 mL | 0.2274 mL | 0.4549 mL | 1.1372 mL | |
| 30 mM | 0.0379 mL | 0.1895 mL | 0.3791 mL | 0.9476 mL | |
| 40 mM | 0.0284 mL | 0.1421 mL | 0.2843 mL | 0.7107 mL | |
| 50 mM | 0.0227 mL | 0.1137 mL | 0.2274 mL | 0.5686 mL | |
| 60 mM | 0.0190 mL | 0.0948 mL | 0.1895 mL | 0.4738 mL | |
| 80 mM | 0.0142 mL | 0.0711 mL | 0.1421 mL | 0.3554 mL | |
| 100 mM | 0.0114 mL | 0.0569 mL | 0.1137 mL | 0.2843 mL |
TD-428 関連分類
HY-114407 関連分類
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