PROTAC AR Degrader-10
PROTAC AR Degrader-10 is a potent cereblon (CRBN)-recruited androgen receptor (AR) PROTAC degrader. PROTAC AR Degrader-10 exhibits high AR degradation activity and can be applied to research related to prostate cancer.
(Pink: Androgen Receptor ligand (HY-173373); Blue: Cereblon ligand (HY-138793); Black: linker).
For research use only. We do not sell to patients.
- Formula: C41H46ClN7O5S
- Molecular Weight:784.37
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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
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CRBN-DDB1 |
In Vitro
PROTAC AR Degrader-10 (GT19) (0.1-500 nM; 24 h) potently degrades androgen receptor in LNCaP human prostate cancer cells, with superior activity compared to Bavdegalutamide (ARV-110) (HY-138641) at concentrations below 100 nM over 24 hours, and obvious degradation at 100 nM over 24 hours[1].
PROTAC AR Degrader-10 binds to human cereblon with high affinity, as measured by an IC50 of 0.15 µM in a cell-free HTRF binding assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP human prostate cancer cells
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Concentration:0.1-500 nM
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Incubation Time:24 h
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Result:Induced high androgen receptor degradation at concentrations below 100 nM over 24 hours.
Caused obvious androgen receptor degradation at a concentration of 100 nM over 24 hours.
Chemical Information
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Molecular Weight 784.37
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Formula C41H46ClN7O5S
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SMILES
ClC1=C(C#N)C=CC(O[C@H]2C(C)(C)[C@H](NC(C3=CC=C(N4CCN(CCCSC5=CC=C(C(N(C6C(NC(CC6)=O)=O)C7)=O)C7=C5)CC4)N=C3)=O)C2(C)C)=C1
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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)