BD-7148
BD-7148 is a potent, highly selective BRD4 PROTAC degrader with a DC50 of 0.9 nM. BD-7148 binds to recombinant human BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1 and BRD4-BD2 domain proteins, with Kd values ranging from 26 nM to 240 nM, and shows no binding preference for BRD4 domains over BRD2 or BRD3 domains. BD-7148 inhibits the growth of leukemia and breast cancer cells. BD-7148 can be used in the research of leukemia and breast cancer.
(Pink: BRD4 Target protein ligand; Blue: Cereblon ligand (HY-41547); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3037514-35-2
- Formula: C37H30N8O5S
- Molecular Weight:698.75
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 0.9 nM (DC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
4.9 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| MCF7 | IC50 |
37.8 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| MDA-MB-231 | IC50 |
15.9 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| MDA-MB-453 | IC50 |
59.9 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-453 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| MOLM-13 | IC50 |
25 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human MOLM-13 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| MV4-11 | IC50 |
17 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| RS4-11 | IC50 |
6.4 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human RS4-11 cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
| T47D | IC50 |
3.3 nM
Compound: 5; BD-7148
|
Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
Antiproliferative activity against human T47D cells assessed as cell growth inhibition incubated for 4 days by WST-8 assay
|
[PMID: 37289649] |
In Vitro
BD-7148 (100 nM; 1200 sec association, 1800 sec dissociation) binds to recombinant human BRD2-BD1, BRD2-BD2, BRD3-BD1, BRD3-BD2, BRD4-BD1, and BRD4-BD2 domain proteins with Kd values ranging from 26 nM to 240 nM, showing no selective binding to BRD4 domains over BRD2 or BRD3 domains[1].
BD-7148 (Up to 1000 nM; 4 h) potently and selectively degrades BRD4 (DC50 = 0.9 nM, Dmax = 99%) with no effect on BRD2 or BRD3 in MV4;11 human acute leukemia cells treated for 4 hours[1].
BD-7148 (Up to 1000 nM; 4 h) potently degrades BRD4 (DC50 = 0.2-13 nM, Dmax = 92-93%) with minimal to no effect on BRD2 and BRD3 in RS4;11, HL-60, and MOLM-13 human acute leukemia cells treated for 4 hours[1].
BD-7148 (Multiple concentrations; 4 day) potently inhibits growth of MV4;11, MOLM-13, HL-60, RS4;11, MDA-MB-231, MDA-MB-453, MCF7, and T47D human cancer cells with IC50 values of 3.3-59.9 nM, and is 8-189 times more potent than QCA276[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:RS4;11, HL60, MOLM-13, MDA-MB-231, MDA-MB-453, MCF7, T47D cells
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Concentration:0, 0.1, 0.3, 1, 3, 10, 100, 300 and 1000 nM
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Incubation Time:4 h
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Result:Degraded BRD4 in RS4;11, HL60, MOLM-13, MDA-MB-231, MDA-MB-453, MCF7, T47D with a DC50 of 0.2, 3.6, 13, 1, 5.6, 3.6 and 0.2 nM.
Chemical Information
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CAS No. 3037514-35-2
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Molecular Weight 698.75
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Formula C37H30N8O5S
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SMILES
O=C1C2=CC=CC(N3CC(C3)N4N=CC(C#CC5=C(CC6=CC=CC=C6)C(COCC7=NN=C(C)N87)=C8S5)=C4)=C2C(N1C9C(NC(CC9)=O)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)