UT-34|cas:2168525-92-4|西域试剂

UT-34,98.01%

产品编号：Bellancom-136242| CAS NO：2168525-92-4| 分子式：C₁₅H₁₂F₄N₄O₂| 分子量：356.27

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-136242	￥1500.00	杭州北京（现货）
Bellancom-136242	￥2500.00	杭州北京（现货）
Bellancom-136242	￥5500.00	杭州北京（现货）
Bellancom-136242	￥9500.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

UT-34

产品介绍

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。

生物活性

UT-34 is a potent, selective and orally active second-generation pan-androgen receptor (AR) antagonist and degrader with IC₅₀s of 211.7 nM, 262.4 nM and 215.7 nM for wild-type, F876L and W741L AR, respectively. UT-34 binds to ligand-binding domain (LBD) and function-1 (AF-1) domains and requires ubiquitin proteasome pathway to degrade the AR. UT-34 has anti-prostate cancer efficacy.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell 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 hours
Result:	Resulted in a reduction of AR levels at 1000 nM.

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal 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 days
Result:	Reduced the seminal vesicle weight.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal 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 days
Result:	Reduced the seminal vesicle weight.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal 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 days
Result:	Reduced the seminal vesicle weight.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (701.71 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8069 mL	14.0343 mL	28.0686 mL
5 mM	0.5614 mL	2.8069 mL	5.6137 mL
10 mM	0.2807 mL	1.4034 mL	2.8069 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.84 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.84 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。