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Chemical Structure : UT-34
CAS No.: 2168525-92-4
Catalog No.: PC-21405Not For Human Use, Lab Use Only.
UT-34 is a potent, second-generation androgen receptor (AR) pan antagonist, degrades enzalutamide-sensitive and -resistant ARs and AR splice variants (AR-SVs).
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|---|---|---|---|
| 10 mg | $198 | In stock | |
| 25 mg | $298 | In stock | |
| 50 mg | $478 | In stock | |
| 100 mg | Get quote |
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UT-34 is a potent, second-generation androgen receptor (AR) pan antagonist, degrades enzalutamide-sensitive and -resistant ARs and AR splice variants (AR-SVs).
UT-34 interacts with AR AF-1 domain, UT-34 does not bind to the AR-LBD.
UT-34 antagonizes the wild-type AR with IC50 of 200 nM, inhibits the various mutant ARs (W741L, T877A, and F876L) comparably or with better IC50.
UT-34 downregulates T877A-AR and F876L-enzalutamide-resistant AR, reduces AR levels at 1 uM in LNCaP and MR49F cells.
UT-34 does not inhibit the transactivation of GR and mineralocorticoid receptor, and does not downregulate the ER and PR protein levels.
UT-34 requires ubiquitin proteasome pathway to degrade the AR.
UT-34 promotes AR-V7 degradation, inhibits AR and AR-V7-target gene expression and induces distinct AR conformation.
UT-34 inhibits enzalutamide-sensitive and -resistant AR-dependent gene expression and prostate cancer cell proliferation.
UT-34 inhibits AR function and proliferation of an AR-amplified model (VCaP cells) and a PDX model.
| M.Wt | 356.28 | |
| Formula | C15H12F4N4O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(αS)-N-[4-Cyano-3-(trifluoromethyl)phenyl]-4-fluoro-α-hydroxy-α-methyl-1H-pyrazole-1-propanamide |
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1. Ponnusamy S, et al. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780.
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