Androgen receptor antagonist 1 - CAS:1338812-36-4

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Androgen receptor antagonist 1

目录号 : KM8655 CAS No. : 1338812-36-4 纯度 : 98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
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50mg		In-stock
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200mg	询价	In-stock

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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.

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

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.

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.

分子量

416.90

CAS号

1338812-36-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。