PROTAC BTK Degrader-12
PROTAC BTK Degrader-12 is a BTK PROTAC degrader that recruits CRBN, with a DC50 of 0.72 nM. PROTAC BTK Degrader-12 achieves ubiquitin-proteasome pathway degradation of BTK by conjugating a BTK inhibitor domain with an E3 ubiquitin ligase ligand domain. PROTAC BTK Degrader-12 can be used in cancer research.
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-W245311); Black: linker (HY-30105)).
For research use only. We do not sell to patients.
- CAS No.: 2736508-65-7
- Formula: C47H54N12O4
- Molecular Weight:851.01
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
Cereblon |
BTK 0.72 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Raji | DC50 |
0.72 nM
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BTK protein degradation in human Burkitt's lymphoma Raji cells measured via Western blotting after 24 h incubation.
BTK protein degradation in human Burkitt's lymphoma Raji cells measured via Western blotting after 24 h incubation.
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en?oq=WO2021219070 |
| Raji | IC50 |
> 10 μM
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Inhibition of BTK kinase activity (measured by reduced phosphorylated BTK levels) in human Burkitt's lymphoma Raji cells via Western blotting after 24 h incubation followed by anti-IgM stimulation.
Inhibition of BTK kinase activity (measured by reduced phosphorylated BTK levels) in human Burkitt's lymphoma Raji cells via Western blotting after 24 h incubation followed by anti-IgM stimulation.
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en?oq=WO2021219070 |
In Vitro
PROTAC BTK Degrader-12 (Example 19) (1-300 nM; 24 h) potently induces dose-dependent degradation of BTK protein in Raji cells, with a DC50 of 0.72 nM[1].
PROTAC BTK Degrader-12 (24 h) potently inhibits BTK kinase activity in Raji cells, with an IC50 > 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2736508-65-7
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Molecular Weight 851.01
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Formula C47H54N12O4
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SMILES
CC(C)(C)C1=NOC(C(N[C@@H](C2=CC=C(C3=C4C(NC(C5=NC=C(N6CCN(CC7CCN(C8=CC=C(N9C(NC(CC9)=O)=O)C=C8)CC7)CC6)C=C5)=C4)=NC=N3)C=C2C)C)=O)=N1
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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)
PROTAC BTK Degrader-12 Related Classifications
HY-170413 Related Classifications
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