UT-155

SKU: orb1308968

Description

UT-155 is a selective and potent androgen receptor (AR) antagonist, exhibiting a binding affinity (Ki) of 267 nM for the AR ligand-binding domain. This small molecule is a valuable research tool for investigating AR signaling in prostate cancer and other androgen-dependent pathologies, applicable in both in vitro and in vivo experimental models.

Research Area

Metabolism Research

Key Properties

• CAS Number: 2031161-35-8
• MW: 405.35
• Purity: 99.63% (May vary between batches)
• Formula: C₂₀H₁₅F₄N₃O₂
• SMILES: C[C@](O)(Cn1ccc2cc(F)ccc12)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F
• Target: Androgen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (9.87 mM);H2O:< 0.1 mg/mL (insoluble);DMSO:130 mg/mL (320.71 mM)

Bioactivity

• Target IC50:
  AR-LBD:267 nM (Ki)
• In Vivo:
  Consistent with its anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenografts by 53%, while enzalutamide has no effect. In UT-155-treated animals, tumor weights, PSA levels, and expression of AR and AR-SV are significantly reduced.
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• In Vitro:
  UT-155 binds to the AR-LBD (Ki: 267 nM) and potently inhibits R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide's efficacy is halved against the W742L mutant AR. In LNCaP cells, UT-155 inhibits PSA and FKBP5 gene expression induced by 0.1 nM R1881 at concentrations between 10 and 100 nM, demonstrating 5-10 times better efficacy than enzalutamide.
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Storage & Handling

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

Alternative Names

UT 155, UT155, UT-155, inhibit, Inhibitor, AR-LBD, androgen receptor, Androgen Receptor, AndrogenReceptor

Compound Identifiers

PubChem CID

122640156