
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)






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Biological Information
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Product NameUT-34
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NoteResearch use only, not for human use.
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Brief DescriptionUT-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.
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DescriptionUT-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.
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In VitroCell 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.
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In VivoAnimal 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.
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetAndrogen Receptor (AR)
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Recptorandrogen receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number2168525-92-4
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Formula Weight356.27
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Molecular FormulaC15H12F4N4O2
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Purity>98% (HPLC)
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SolubilityDMSO:71 mg/mL (199.29 mM)
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SMILESC[C@](O)(Cn1cc(F)cn1)C(=O)Nc1ccc(C#N)c(c1)C(F)(F)F
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference



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Nilutamide
Nilutamide is an antineoplastic hormonal agent primarily used in the treatment of prostate Y. Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors).
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ACP-105
ACP-105 is a novel and potent nonsteroidal selective androgen receptor modulator (SARM) with partial agonist activity relative to the natural androgen testosterone.
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Dimethylcurcumin
Dimethylcurcumin (ASC-J9) is an androgen receptor degradation enhancer. It effectively suppresses castration-resistant prostate cancer cell proliferation and invasion.Dimethylcurcumin is able to degrade fAR and AR3 in a dose-dependent manner in various human PCa cells. Dimethylcurcumin can also effectively suppress AR-targeted genes in CWR22Rv1-fARKD cells.