TargetMol

Androgen receptor antagonist 1

Product Code:
 
TAR-T10320
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T10320-5mg5mg£370.00
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TAR-T10320-50mg50mg£1,661.00
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Quantity:
TAR-T10320-100mg100mg£2,079.00
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Further Information

Bioactivity:
Androgen receptor antagonist 1 is an orally available full androgen receptor antagonist (IC50: 59 nM). It can be used in the synthesis of PROTAC AR degraders, which results in 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
CAS:
1338812-36-4
Formula:
C21H25ClN4O3
Molecular Weight:
416.91
Purity:
0.98
SMILES:
CC1(C)[C@H](NC(=O)c2cnn(CCO)c2)C(C)(C)[C@H]1Oc1ccc(C#N)c(Cl)c1

References

1. Guo C, et al. Discovery of aryloxy tetramethylcyclobutanes as novel androgen receptor antagonists. J Med Chem. 2011 Nov 10;54(21):7693-704. 2. Han X, et al. 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 24;62(2):941-964.