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UT-34 

Cat. No.: HY-136242
Handling Instructions

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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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].

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].

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.

2168525-92-4

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

UT-34UT34UT 34Androgen ReceptorARprostatecancerligand-bindingfunction-1degraderARVsenzalutamideubiquitinproteasomeFKBP5Inhibitorinhibitorinhibit

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UT-34
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