3064715-04-1
Chemical Structure
AR antagonist 17
- CAS No.: 3064715-04-1
- Formula:C21H20F3N3O4S2
- Molecular Weight:499.53
InChIKey: GWYPGKZILPDBDS-UHFFFAOYSA-N
SMILES: CC1=C(C=C(O1)C2=CC=CC(C(F)(F)F)=C2)C(NC3=NC(CN4CCS(=O)(CC4)=O)=CS3)=O
Biological Activity: AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC)[1].
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AR antagonist 17 | AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC). | |||||||||||||||||||||
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