Home Endocrinology & Hormones Androgen Receptor antagonist UT-34 For research use only.

UT-34

UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.

UT-34 Chemical Structure

UT-34 Chemical Structure

CAS: 2168525-92-4

Purity & Quality Control

Batch: S888501 DMSO] 71 mg/mL] false] Ethanol] 71 mg/mL] false] Water] Insoluble] false Purity: 99.05%
99.05

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Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

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Biological Activity

Description UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer.
Targets
AR-T877A [1]
(Cell-free assay)		 AR-W741L [1]
(Cell-free assay)		 AR-WT [1]
(Cell-free assay)
80.78 nM 94.17 nM 203.46 nM
In vitro
In vitro

UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vitro proliferation. UT-34 promotes a conformation that is distinct from the LBD-binding competitive antagonist enzalutamide and degrades the AR through the ubiquitin proteasome mechanism. UT-34 has a broad safety margin and exhibits no cross-reactivity with Gprotein-coupled receptor kinase and nuclear receptor family members.[1]
Cell Research Cell lines LNCaP, PC-3, HEK-293, ZR-75-1, MDA-MB-453, VCaP, 22RV1, and COS7 cell lines
Concentrations 0.1 μM, 1 μM, 10 μM
Incubation Time 30 min, 24 h, 48 h
Method

LNCaP cells are maintained in 1% charcoal-stripped serum-containing mediumfor two days. Cells are treated with the indicated doses of UT-34 in the presence of 0.1 nmol/L R1881 for 24 hours, protein is extracted, and Western blot analysis for AR and actin is performed.
In Vivo
In vivo

UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vivo growth of enzalutamide-sensitive and -resistant prostate cancer xenografts. In preclinical models, UT-34 induces the regression of enzalutamide-resistant tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors.[1]
Animal Research Animal Models NSG mice with MR49F xenograft
Dosages 20 mg/kg, 40 mg/kg
Administration Oral gavage

Chemical Information & Solubility

Molecular Weight 356.27 Formula

C15H12F4N4O2
CAS No. 2168525-92-4 SDF --
Smiles CC(CN1C=C(C=N1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (199.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 71 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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