TargetMol

ARD-69

Product Code:
 
TAR-T30123
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20°C
1 / 1
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Further Information

Bioactivity:
ARD-69 is a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. ARD-69 induces degradation of AR protein in AR-positive prostate cancer cell lines in a dose- and time-dependent manner. ARD-69 achieves DC50 values of 0.86, 0.76, and 10.4 nM in LNCaP, VCaP, and 22Rv1 AR+ prostate cancer cell lines, respectively. ARD-69 is capable of reducing the AR protein level by >95% in these prostate cancer cell lines and effectively suppressing AR-regulated gene expression.
CAS:
T30123
Molecular Weight:
1129.83
Purity:
0.98
SMILES:
O=C([C@H]1N(C([C@@H](NC(C2(F)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)N[C@H](C3=CC=C(C4=C(C)N=CS4)C=C3)CC(N5CCC(N6CCC(C#CC7=CC=C(C(N[C@H]8C(C)(C)[C@H](OC9=CC=C(C#N)C(Cl)=C9)C8(C)C)=O)C=C7)CC6)CC5)=O

References

Han X, Wang C, Qin C, Xiang W, Fernandez-Salas E, Yang CY, Wang M, Zhao L, Xu T, Chinnaswamy K, Delproposto J, Stuckey J, Wang S. Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer. J Med Chem. 2019 Jan 10. doi: 10.1021/acs.jmedchem.8b01631. [Epub ahead of print] PubMed PMID: 30629437.