| 名称 | UT-34 |
| 描述 | 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. |
| 体外活性 | 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[1].In LNCaP cells UT-34 (0.1-10 μM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM [1]. 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[1]. 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[1]. |
| 体内活性 | 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 [1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 71 mg/mL (199.29 mM)
|
| 关键字 | enzalutamide | Inhibitor | Androgen Receptor | UT34 | inhibit | ubiquitin | FKBP5 | cancer | prostate | UT-34 | proteasome | degrader | ARVs | UT 34 | function-1 | ligand-binding |
| 相关产品 | Dehydroisoandrosterone 3-acetate | Bicalutamide | 2,2,5,7,8-Pentamethyl-6-Chromanol | S-23 | Bavdegalutamide | Enzalutamide | Adrenosterone | Allura Red AC | SK33 | Sunset Yellow FCF | Ostarine | Flutamide |
| 相关库 | 核受体化合物库 | 经典已知活性库 | 抑制剂库 | 内分泌激素分子库 | 抗前列腺癌化合物库 | 口服活性化合物库 | 已知活性化合物库 | 抗癌化合物库 | 抗癌活性化合物库 | 转录因子库 |
United States
