2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. UT-34

UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.

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UT-34 Chemical Structure

UT-34 Chemical Structure

CAS No. : 2168525-92-4

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Based on 1 publication(s) in Google Scholar

UT-34 Related Antibodies

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Description

UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy[1][2].

IC50 & Target

IC50: 211.7 nM (Wild-type AR), 262.4 nM (F876L AR) and 215.7 nM (W741L AR)[1]
In Vitro

UT-34 (3-10 µM; 24 hours; LNCaP cells) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM[1].
UT-34 (0.1-10 µM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM in LNCaP cells[1].
Treatment of ZR-75-1 cells maintained in serum-containing growth medium with UT-34 results in downregulation of AR protein levels, but not estrogen receptor (ER) or progesterone receptor (PR) levels. Furthermore, in MDA-MB-453 breast cancer cells that express AR and glucocorticoid receptor (GR), UT-34 induces the downregulation of AR, but not GR[1].
UT-34 is an effective degrader of both AR and AR-V7. LNCaP-ARV7 cells are treated for 24 hours in the presence of 0.1 nM R1881 or 10 ng/mL Doxycycline. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, while UT-34 inhibits the expression of R1881-induced FKBP5 gene expression[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

UT-34 Related Antibodies

Cell Viability Assay[1]

Cell Line: LNCaP cells
Concentration: 3 µM, 10 µM
Incubation Time: 24 hours
Result: Inhibited the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.1 µM, 1 µM, 10 µM
Incubation Time: 24 hours
Result: Resulted in a reduction of AR levels at 1000 nM.
In Vivo

UT-34 (20-40 mg/kg; oral administration; daily; for 14 days; NSG mice) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively[1].
UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles in rats, and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. UT-34 also induces tumor regression in intact immunocompromised rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Non obese diabetic/severe combined immunodeficiency Gamma (NSG) mice injected with MR49F cells[1]
Dosage: 20 mg/kg or 40 mg/kg
Administration: Oral administration; daily; for 14 days
Result: Reduced the seminal vesicle weight.
Molecular Weight

356.27

Formula

C15H12F4N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)[C@@](C)(O)CN2N=CC(F)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (701.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8069 mL 14.0343 mL 28.0686 mL
5 mM 0.5614 mL 2.8069 mL 5.6137 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8069 mL 14.0343 mL 28.0686 mL 70.1715 mL
5 mM 0.5614 mL 2.8069 mL 5.6137 mL 14.0343 mL
10 mM 0.2807 mL 1.4034 mL 2.8069 mL 7.0172 mL
15 mM 0.1871 mL 0.9356 mL 1.8712 mL 4.6781 mL
20 mM 0.1403 mL 0.7017 mL 1.4034 mL 3.5086 mL
25 mM 0.1123 mL 0.5614 mL 1.1227 mL 2.8069 mL
30 mM 0.0936 mL 0.4678 mL 0.9356 mL 2.3391 mL
40 mM 0.0702 mL 0.3509 mL 0.7017 mL 1.7543 mL
50 mM 0.0561 mL 0.2807 mL 0.5614 mL 1.4034 mL
60 mM 0.0468 mL 0.2339 mL 0.4678 mL 1.1695 mL
80 mM 0.0351 mL 0.1754 mL 0.3509 mL 0.8771 mL
100 mM 0.0281 mL 0.1403 mL 0.2807 mL 0.7017 mL
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UT-34 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UT-342168525-92-4UT34UT 34Androgen ReceptorARprostatecancerligand-bindingfunction-1degraderARVsenzalutamideubiquitinproteasomeFKBP5Inhibitorinhibitorinhibit

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