Androgen receptor antagonist 1|cas:1338812-36-4|西域试剂

Androgen receptor antagonist 1,99.39%

产品编号：Bellancom-130992| CAS NO：1338812-36-4| 分子式：C₂₁H₂₅ClN₄O₃| 分子量：416.90

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货号	价格	库存与货期
Bellancom-130992	￥4500.00	杭州北京（现货）
Bellancom-130992	￥8000.00	杭州北京（现货）
Bellancom-130992	￥15500.00	杭州北京（现货）
Bellancom-130992	￥23500.00	杭州北京（现货）

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Androgen receptor antagonist 1

产品介绍

Androgen receptor antagonist 1 是一种口服有效的完整雄激素受体 (AR) 拮抗剂，IC₅₀ 为 59 nM。Androgen receptor antagonist 1 可用于合成 PROTAC AR 降解剂，1 μM 和 10 μM PROTAC AR 降解剂作用于 LNCaP 细胞，分别导致 24% 和 47% AR 蛋白降解。

生物活性

Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC₅₀ of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.

体外研究

Androgen receptor antagonist 1 (Compound 26; 1 nM-100 μM) shows significant cell growth inhibition effects for LNCaP and LNAR cells but not DU145 cells.

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

Cell Proliferation Assay

Cell Line:	Prostate cancer (CaP) cells (LNCAP, LNAR, and DU145)
Concentration:	1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM
Incubation Time:	7 days
Result:	Antiproliferative effects of in LNCAP and LNAR cells.

体内研究
(In Vivo)

Androgen receptor antagonist 1 (Compound 26; 100 mg/kg once a day for 5 weeks) demonstrates excellent in vivo tumor growth inhibition upon oral administration in a castration-resistant prostate cancer (CRPC) animal model.

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

Animal Model:	Male athymic nude mice with LNCaP xenograft model of CRPC
Dosage:	100 mg/kg
Administration:	Orally once a day for 5 weeks
Result:	Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.

体内研究

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

Animal Model:	Male athymic nude mice with LNCaP xenograft model of CRPC
Dosage:	100 mg/kg
Administration:	Orally once a day for 5 weeks
Result:	Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.

体内研究

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

Animal Model:	Male athymic nude mice with LNCaP xenograft model of CRPC
Dosage:	100 mg/kg
Administration:	Orally once a day for 5 weeks
Result:	Demonstrated outstanding efficacy in inhibiting tumor growth. At the given doses (100 mg/kg once a day) nearly completely suppressed tumor growth (by 90 %) and the PSA levels (78%) after 5 weeks, with no detectable body weight loss for the period of time when animals were treated.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (239.87 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3987 mL	11.9933 mL	23.9866 mL
5 mM	0.4797 mL	2.3987 mL	4.7973 mL
10 mM	0.2399 mL	1.1993 mL	2.3987 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 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.00 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.00 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。