UT-34

SKU: orb1308967

Description

UT-34 is a potent, orally bioavailable pan-androgen receptor antagonist and degrader effective against wild-type and mutant (F876L, W741L) AR. It demonstrates anti-tumor activity in prostate cancer models, making it a valuable research tool for investigating AR signaling and therapeutic resistance in both in vitro and in vivo studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2168525-92-4
• MW: 356.27
• Purity: 98.12% (May vary between batches)
• Formula: C₁₅H₁₂F₄N₄O₂
• SMILES: C[C@](O)(Cn1cc(F)cn1)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F
• Target: Androgen Receptor,Estrogen Receptor/ERR
• Solubility: DMSO:71 mg/mL (199.29 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.61 mM)

Bioactivity

• Target IC50:
  W741L AR:215.7 nM |AR (wild-type):211.7 nM |F876L AR:262.4 nM
• In Vivo:
  In NSG mice, UT-34 (20-40 mg/kg; oral administration; daily; for 14 days ) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively. in rats,UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles , and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. In intact immunocompromised rats, UT-34 also induces tumor regression .
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• In Vitro:
  In LNCaP cells, UT-34 (3-10 μM; 24 hours) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.In LNCaP cells UT-34 (0.1-10 μM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM . 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. UT-34 is an effective degrader of both AR and AR-V7.LNCaP-ARV7 cells were treated in the presence of 0.1 nM R1881 or 10 ng/mL doxycycline for 24 hours. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, and UT-34 inhibits the expression of FKBP5 gene expression induced by R1881.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

degrader, cancer, ARVs, AndrogenReceptor, Androgen Receptor, androgen receptor, FKBP5, F876L AR, function-1, enzalutamide, ligand-binding, Inhibitor, inhibit, ubiquitin, UT 34, UT34, UT-34, W741L AR, proteasome, prostate, Wild-type AR

Compound Identifiers

PubChem CID

132214622