UT-34
规格
| Cas Number | 2168525-92-4 |
| 规格或纯度 | 10mM in DMSO |
| 包装 | 1ml |
产品信息
| 品牌 | 阿拉丁 |
| 浓度 | 10mM in DMSO |
| 简短描述 | 雄激素受体拮抗剂 |
| 英文简短描述 | Androgen Receptor Antagonists |
| 过滤标签 | Compound libraries |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | UT-34是一种强效、选择性和口服生物利用度高的第二代雄激素受体（AR）泛拮抗剂和降解剂，对野生型、T877A和W741L AR的IC50分别为203.46 nM、80.78 nM和94.17 nM。UT-34是治疗恩杂鲁胺耐药前列腺癌的潜在新一代疗法。 |
| 英文描述 |
Information UT-34 UT-34 is a potent, selective and orally bioavailable second-generation androgen receptor (AR) pan antagonist and degrader with IC50 of 203.46 nM, 80.78 nM and 94.17 nM for wild-type, T877A and W741L AR, respectively. UT-34 is a potential next-generation therapeutic for enzalutamide-resistant prostate cancer. Targets AR-T877A (Cell-free assay); AR-W741L (Cell-free assay); AR-WT (Cell-free assay) 80.78 nM; 94.17 nM; 203.46 nM In vitro UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vitro proliferation. UT-34 promotes a conformation that is distinct from the LBD-binding competitive antagonist enzalutamide and degrades the AR through the ubiquitin proteasome mechanism. UT-34 has a broad safety margin and exhibits no cross-reactivity with Gprotein-coupled receptor kinase and nuclear receptor family members. In vivo UT-34 inhibits the wild-type and LBD-mutant ARs comparably and inhibits the in vivo growth of enzalutamide-sensitive and -resistant prostate cancer xenografts. In preclinical models, UT-34 induces the regression of enzalutamide-resistant tumors at doses when the AR is degraded; but, at lower doses, when the AR is just antagonized, it inhibits, without shrinking, the tumors. Cell Research(from reference) Cell lines：LNCaP, PC-3, HEK-293, ZR-75-1, MDA-MB-453, VCaP, 22RV1, and COS7 cell lines Concentrations：0.1 μM, 1 μM, 10 μM Incubation Time：30 min, 24 h, 48 h |