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).
For research use only. We do not sell to patients.
- Purity: 98.81%
- CAS No.: 2334525-50-5
- Formula: C43H43ClN10O7S
- Molecular Weight:879.38
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Storage: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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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.
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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.
|
j.ejmech.2019.01.023. |
In Vitro
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).
Chemical Information
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CAS No. 2334525-50-5
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Appearance Solid
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Molecular Weight 879.38
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (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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Handling Instructions (2659 KB)
References
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 |
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| 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 Related Classifications
HY-114407 Related Classifications
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