PROTAC AR Degrader-11
PROTAC AR Degrader-11 is a PROTAC degrader that targets the androgen receptor (AR) and its splice variant AR-V7. PROTAC AR Degrader-11 simultaneously degrades full-length AR and AR-V7 via the ubiquitin-proteasome system by recruiting the CRL4-CRBN E3 ligase (FIG.2A). PROTAC AR Degrader-11 reduces the viability of cancer cells. PROTAC AR Degrader-11 can be used in studies related to castration-resistant prostate cancer.
(Pink: Androgen Receptor ligand (HY-171809); Blue: Cereblon ligand (HY-A0003); Black: linker (HY-169966)).
For research use only. We do not sell to patients.
- CAS No.: 2798907-41-0
- Formula: C36H39F3N8O6
- Molecular Weight:736.74
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
More
Biological Activity
Description
IC50 & Target
[1]|
AR-V7 |
In Vitro
PROTAC AR Degrader-11 (Compound 30) (10-10000 nM; 3-7 days) reduces the viability of castration-resistant prostate cancer cells expressing androgen receptor/AR-V7 in a concentration- and time-dependent manner[1].
PROTAC AR Degrader-11 reduces full-length AR and AR-V7 protein levels in a concentration-dependent manner in CWR22RV1 (AR-V7 high-expression) and VCaP (AR-amplified) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:castration-resistant prostate cancer cells expressing androgen receptor/AR-V7
-
Concentration:10, 100, 1000 and 10000 nM
-
Incubation Time:3 days; 7 days
-
Result:Resulted in ~110% cell viability at 10 nM, ~52% at 100 nM, ~27% at 1000 nM, and ~20% at 10000 nM after 3 days incubation.
Resulted in ~102% cell viability at 10 nM, ~32% at 100 nM, ~3% at 1000 nM, and ~2% at 10000 nM after 7 days incubation.
Chemical Information
-
CAS No. 2798907-41-0
-
Molecular Weight 736.74
-
Formula C36H39F3N8O6
-
SMILES
O=C(COCCCCOC1=CC=C(C2CCN(CC2)C3=NN4C(CC3)=NN=C4C(F)(F)F)C=C1)NC5=CC=CC6=C5CN(C7C(NC(CC7)=O)=O)C6=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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)