货号	规格	价格	上海	北京	珠海	重庆	武汉
S89769-5mg买3赠1	≥98%	￥765.00 S89769-5mg ￥765.00 现货（买3赠1）	100 >10	-	-	-	-
S89769-10mg买3赠1	≥98%	￥1360.00 S89769-10mg ￥1360.00 现货（买3赠1）	50 >10	-	-	-	-
S89769-25mg买3赠1	≥98%	￥2720.00 S89769-25mg ￥2720.00 现货（买3赠1）	20 >10	-	-	-	-
S89769-100mg	≥98%	￥6590.00 S89769-100mg ￥6590.00 现货	5 5	-	-	-	-

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产品描述：

UT-34 是一种有效的，选择性的，具有口服活性的第二代泛雄激素受体 (AR) 拮抗剂和降解剂，对野生型 AR，F876L-AR 和 W741L-AR 的 IC50 分别为 211.7 nM，262.4 nM 和 215.7 nM。UT-34 与配体结合结构域 (LBD) 和功能 1 (AF-1) 结构域结合，并需要泛素蛋白酶体途径来降解 AR。UT-34 具有抗前列腺癌的功效。

靶点：

IC50: 211.7 nM (Wild-type AR), 262.4 nM (F876L AR) and 215.7 nM (W741L AR);AndrogenReceptor

体外研究：

UT-34 (3-10 µM; 24 hours; LNCaP cells) treatment inhibits the expression of PSA and FKBP5 and growth of LNCaP cells starting from 100 nM with maximum effect observed at 10 μM.
UT-34 (0.1-10 µM; 24 hours; LNCaP cells) treatment results in a reduction of AR levels at 1000 nM in LNCaP cells.
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 are treated for 24 hours in the presence of 0.1 nM R1881 or 10 ng/mL Doxycycline. Doxycycline induces the expression of EDN2, which is inhibited by UT-34, while UT-34 inhibits the expression of R1881-induced FKBP5 gene expression.

体内研究：

UT-34 (20-40 mg/kg; oral administration; daily; for 14 days; NSG mice) at 20 and 40 mg/kg reduces the seminal vesicle weight by 10%-20% and 50%-60 %, respectively.
UT-34 inhibits androgen-dependent tissues such as prostate and seminal vesicles in rats, and the growth of Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenografts. UT-34 also induces tumor regression in intact immunocompromised rats.

参考文献：

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.
2. Stone L. UT-34: a promising new AR degrader. Nat Rev Urol. 2019 Nov;16(11):640.

溶解性：

soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.807 ml	14.034 ml	28.069 ml
5 mM	0.561 ml	2.807 ml	5.614 ml
10 mM	0.281 ml	1.403 ml	2.807 ml
50 mM	0.056 ml	0.281 ml	0.561 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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