TD-428
Based on 1 Customer Validation
TD-428 is a PROTAC connected by ligands for Cereblon and BRD4. TD-428 is a highly specific BRD4 degrader with a DC50 of 0.32 nM. TD-428 is a BET PROTAC, which comprises TD-106 (a CRBN ligand) linked to JQ1 (a BET inhibitor). TD-428 efficiently induce BET protein degradation.
(Pink: BRD4 ligand (HY-78695); Blue: Cereblon ligand (HY-114406); Black: linker).
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- Pureté: 98.81%
- CAS No.: 2334525-50-5
- Formule: C43H43ClN10O7S
- Masse moléculaire:879.38
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Stockage: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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Activité biologique
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BRD4 0.32 nM (DC50) |
Cereblon |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | CC50 |
20.1 nM
Compound: TD-428; 21b
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Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
Antiproliferative activity against human 22Rv1 cells after 72 hrs by CelTiter-Glo reagent-based luminescence assay
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[PMID: 30684871] |
TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1[1].
TD-428 (0.01-10,000 nM; 72 hours) inhibits the proliferation of 22RV1 cells with a CC50 of 20.1 nM[1].
TD-428 (1 nM-10 μM; 12 hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:22RV1 cells
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Concentration:0.01, 0.1, 1, 10, 100, 1000, and 10000 nM
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Incubation Time:72 hours
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Result:Inhibited cell proliferation with a CC50 of 20.1 nM.
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Cell Line:U266 cells
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Concentration:1 nM, 10 nM, 100 nM, 1000 nM, and 10 μM
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Incubation Time:12 hours
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Result:Induced the degradation of BRD4, IKZF1, IKZF3 proteins.
Chemical Information
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CAS No. 2334525-50-5
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Appearance Solid
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Masse moléculaire 879.38
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Formule 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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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
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)
Pureté et documentation
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Fiche technique (273 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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Instruction de manipulation (2659 KB)
Références
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 Related Classifications
HY-114407 Related Classifications
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