UT-34

CAS No. 2168525-92-4

UT-34( —— )

Catalog No. M22452 CAS No. 2168525-92-4

UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy. 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.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    UT-34
  • Note
    Research use only, not for human use.
  • Brief Description
    UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy. 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.
  • Description
    UT-34 is a selective and orally active antagonist of second-generation pan-androgen receptor (AR) and degrader(IC50s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively), and has anti-prostate cancer efficacy. 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.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[1]. 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.
  • In Vitro
    Cell Viability Assay 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 Cell Line:LNCaP cells Concentration:0.1 μM, 1 μM, 10 μM Incubation Time:24 hoursResult:Resulted in a reduction of AR levels at 1000 nM.
  • In Vivo
    Animal Model:Non obese diabetic/severe combined immunodeficiency Gamma (NSG) mice injected with MR49F cells Dosage:20 mg/kg or 40 mg/kg Administration:Oral administration; daily; for 14 daysResult:Reduced the seminal vesicle weight.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    Androgen Receptor (AR)
  • Recptor
    androgen receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2168525-92-4
  • Formula Weight
    356.27
  • Molecular Formula
    C15H12F4N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:71 mg/mL (199.29 mM)
  • SMILES
    C[C@](O)(Cn1cc(F)cn1)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.
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