UT-155

SKU: orb1218510

Description

UT-155 is a selective and potent antagonist of the androgen receptor (AR) (Ki: 267 nM for UT-155 binding to AR-LBD).

Key Properties

• CAS Number: 2031161-35-8
• MW: 405.35
• Purity: >98% (HPLC)
• Formula: C₂₀H₁₅F₄N₃O₂
• SMILES: C[C@](Cn(cc1)c(cc2)c1cc2F)(C(Nc(cc1)cc(C(F)(F)F)c1C#N)=O)O
• Target: Androgen Receptor (AR)
• Solubility: DMSO:130 mg/mL (320.71 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• In Vivo:
  Consistent with the anti-proliferative effects in vitro, UT-155 significantly inhibits the growth of 22RV1 xenograft by 53%, while, as expected, enzalutamide has no effect on the growth of the 22RV1 tumors. Tumor weights and PSA and the expression of AR and AR-SV are significantly lower in UT-155-treated animals.
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• In Vitro:
  UT-155 binds to the AR-LBD at Ki of 267 nM. UT-155 potently inhibits the R1881-induced wildtype AR transactivation with 6-10-fold higher potency than enzalutamide. While UT-155 antagonizes both wildtype and mutant ARs comparably, enzalutamide is weaker by two fold with the W742 L mutant AR relative to the wild type AR. Treatment of LNCaP cells with UT-155 inhibits 0.1 nM R1881-induced PSA and FKBP5 gene expression between 10 and 100 nM with 5-10-fold better potency than enzalutamide.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Androgen Receptor (AR)