UT-34

Catalog No.S8885

For research use only.

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

CAS No. 2168525-92-4

Purity & Quality Control

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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

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]

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]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: NSG mice with MR49F xenograft
  • Dosages: 20 mg/kg, 40 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 71 mg/mL
(199.28 mM)
Ethanol 71 mg/mL
(199.28 mM)
Water Insoluble

Chemical Information

Molecular Weight 356.27
Formula

C15H12F4N4O2

CAS No. 2168525-92-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(CN1C=C(C=N1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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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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