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 t
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包装价格促销价数量
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5mg￥1625.001300.00- +
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10mg￥2725.002180.00- +
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25mg￥5937.004750.00- +
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50mg￥10250.008200.00- +
- 货号: ajcx33100
- CAS: 2168525-92-4
- 别名:
- 分子式: C15H12F4N4O2
- 分子量: 356.27
- 纯度: ＞98%
- 溶解度: DMSO : 250 mg/mL (701.71 mM; Need ultrasonic)
- 储存: Store at -20°C
- 库存: 现货
Background
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.
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.[1]
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.[1]
[1] Suriyan Ponnusamy, et al. Clin Cancer Res. 2019 Nov 15;25(22):6764-6780.
