UT-34
Based on 1 Customer Validation
UT-34 is a potent, selective, orally bioactive second-generation pan-androgen receptor (AR) antagonist and degrader, with IC50 values of 211.7 nM, 262.4 nM, and 215.7 nM for wild-type AR, F876L-AR, and W741L-AR, respectively. UT-34 binds to the ligand-binding domain (LBD) and functional 1 (AF-1) domain of AR and requires the ubiquitin-proteasome pathway for AR degradation. UT-34 has anti-prostate cancer effects.
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- Purity: 98.09%
- CAS No.: 2168525-92-4
- 화학식: C15H12F4N4O2
- 분자량:356.27
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Anti-Cancer Compound Library
HY-L025
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Endocrinology Compound Library
HY-L047
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Prostate Cancer Compound Library
HY-L124
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Nuclear Receptor Compound Library
HY-L126
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Heterocyclic Compound Library
HY-L138
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Membrane Receptor-targeted Compound Library
HY-L150
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
IC50: 211.7 nM (Wild-type AR), 262.4 nM (F876L AR) and 215.7 nM (W741L AR)[1]
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Cell Line
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Type | Value | Description | References |
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| CWR22R | IC50 |
12.9 μM
Compound: UT34
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Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
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[PMID: 38512060] |
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.
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Cell Line:LNCaP cells
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Concentration:3 µM, 10 µM
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Incubation Time:24 hours
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Result:Inhibited the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.
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Cell Line:LNCaP cells
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Concentration:0.1 µM, 1 µM, 10 µM
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Incubation Time:24 hours
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Result:Resulted in a reduction of AR levels at 1000 nM.
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.
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Animal Model:Non obese diabetic/severe combined immunodeficiency Gamma (NSG) mice injected with MR49F cells[1]
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Dosage:20 mg/kg or 40 mg/kg
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Administration:Oral administration; daily; for 14 days
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Result:Reduced the seminal vesicle weight.
Chemical Information
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CAS No. 2168525-92-4
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Appearance Solid
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분자량 356.27
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화학식 C15H12F4N4O2
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Color White to off-white
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SMILES
O=C(NC1=CC=C(C#N)C(C(F)(F)F)=C1)[C@@](C)(O)CN2N=CC(F)=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Ponnusamy S, et al. Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780. [Content Brief]
[2]. Stone L. UT-34: a promising new AR degrader. Nat Rev Urol. 2019 Nov;16(11):640. [Content Brief]
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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