BTR2004
Based on 1 Customer Validation
BTR2004 is a potent and selective BET family (BRD2/3/4) PROTAC degrader, with EC50 values of 46, 87, and 777 nM, respectively. By bridging BET family proteins and the CUL3-KLHL20 E3 ubiquitin ligase, BTR2004 forms a ternary complex in the nucleus, thereby mediating the degradation of target proteins via the ubiquitin-proteasome system. BTR2004 can be used in research related to prostate cancer, breast cancer, colorectal cancer, osteosarcoma, and hepatocellular carcinoma.
(Pink: BET ligand (HY-161125); Blue: KLHL20 ligand (HY-172563); Black: linker (HY-W015236)).
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 3093583-69-5
- Formula: C54H66ClN13O11S3
- Molecular Weight:1204.83
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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
Biological Activity
Description
IC50 & Target
[1]|
BRD2 46 nM (EC50) |
BRD3 87 nM (EC50) |
BRD4 777 nM (EC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | EC50 |
46 nM
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Degradation of BRD2 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
Degradation of BRD2 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
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36328355 |
| PC-3 | EC50 |
87 nM
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Degradation of BRD3 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
Degradation of BRD3 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
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36328355 |
| PC-3 | EC50 |
777 nM
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Degradation of BRD4 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
Degradation of BRD4 in human PC3 cells assessed via Western blot data fitting to a sigmoid 3-parameter model.
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36328355 |
In Vitro
BTR2004 (62.5 nM-10 μM; 4 h) dose-dependently degrades BRD2, BRD3, and BRD4 proteins in PC3 cells, with EC50 values of 46, 87, and 777 nM, respectively; it degrades nuclear BRD3 protein in the nuclear fraction of PC3 cells; and it degrades BRD3 protein in MDA-MB-231, HCT116, CAPAN-2, HepG2, and U2OS cells[1].
BTR2004 (1.25-10 μM; 24-96 h) inhibits cell proliferation in PC3, MDA-MB-231 and HepG2 cells, and exhibits low cytotoxicity in the normal human cell line hTERT-BJ1[1].
BTR2004 (2-8 μM; 45 min-3 h) induces time-dependent degradation of BRD2 and BRD4 via the ubiquitin-proteasome pathway in U2OS T-REx cells[2].
BTR2004 (12 μM; 3 h) acts to form a KLHL20-BTR2004-BRD4 ternary complex in the nucleus of U2OS T-REx cells expressing HA-KLHL20[2].
BTR2004 retains the ability to degrade BRD2 in U2OS T-REx cells even in the presence of the nuclear export inhibitor KPT276 (HY-17539)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC3 cells
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Concentration:62.5 nM, 125 nM, 250 nM, 500 nM, 1 μM, 2 μM, 10 μM
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Incubation Time:4 h
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Result:Degraded BRD2, BRD3, and BRD4 proteins, as well as BRD3 protein in the nuclear fraction.
Degraded BRD2, BRD3, and BRD4 proteins in a dose-dependent manner.
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Cell Line:MDA-MB-231, HCT116, U2OS, CAPAN-2, HepG2 cells
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Concentration:10 μM (MDA-MB-231, HCT116, U2OS); 5 μM (CAPAN-2, HepG2)
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Incubation Time:4 h
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Result:Degraded BRD3 protein.
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Cell Line:PC3, MDA-MB-231, HepG2, hTERT-BJ1 cells
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Concentration:1.25 μM, 2.5 μM, 5 μM, 10 μM
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Incubation Time:24, 72, 96 h
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Result:Significantly inhibited the growth and proliferation of cancer cells.
Exhibited low cytotoxicity to hTERT-BJ1 normal human cell line.
Chemical Information
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CAS No. 3093583-69-5
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Appearance Solid
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Molecular Weight 1204.83
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Formula C54H66ClN13O11S3
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Color White to off-white
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SMILES
CC1=NN=C2N1C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NCC(NCC(NCC(N[C@H](C(N5[C@H](C(N[C@@H](CC(O)=O)C(N[C@@H](CC(C)C)C(N[C@H](C(N)=O)CSC6)=O)=O)=O)CCC5)=O)CSCC7=CC=CC6=C7)=O)=O)=O)=O
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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 (83.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (294 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.8300 mL | 4.1500 mL | 8.2999 mL | 20.7498 mL |
| 5 mM | 0.1660 mL | 0.8300 mL | 1.6600 mL | 4.1500 mL | |
| 10 mM | 0.0830 mL | 0.4150 mL | 0.8300 mL | 2.0750 mL | |
| 15 mM | 0.0553 mL | 0.2767 mL | 0.5533 mL | 1.3833 mL | |
| 20 mM | 0.0415 mL | 0.2075 mL | 0.4150 mL | 1.0375 mL | |
| 25 mM | 0.0332 mL | 0.1660 mL | 0.3320 mL | 0.8300 mL | |
| 30 mM | 0.0277 mL | 0.1383 mL | 0.2767 mL | 0.6917 mL | |
| 40 mM | 0.0207 mL | 0.1037 mL | 0.2075 mL | 0.5187 mL | |
| 50 mM | 0.0166 mL | 0.0830 mL | 0.1660 mL | 0.4150 mL | |
| 60 mM | 0.0138 mL | 0.0692 mL | 0.1383 mL | 0.3458 mL | |
| 80 mM | 0.0104 mL | 0.0519 mL | 0.1037 mL | 0.2594 mL |
BTR2004 Related Classifications
HY-172562 Related Classifications
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