Androgen receptor antagonist 1

CAS: 1338812-36-4 货号: A649713 分子式: C21H25ClN4O3 分子量: 416.90
有货
级别和纯度: ≥99%
储存条件
-20°C储存
运输条件
超低温运输
★
规格
库存
价格
数量
10mg
A649713-10mg
期货 Stock Image
¥8,000.90
25mg
A649713-25mg
期货 Stock Image
¥15,500.90
50mg
A649713-50mg
期货 Stock Image
¥23,500.90
5mg
A649713-5mg
期货 Stock Image
¥4,500.90
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为什么选择此级别

提供 ≥99% 纯度,适用于对基线干扰要求严格的色谱和分析工作流程。

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储存与运输

-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。

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质量文档

SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Androgen receptor antagonist 1 is an orally available full androgen receptor ( AR ) antagonist with an IC 50 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 .

In Vitro

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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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.

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 . MCE 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.

Form:Solid

IC50& Target:IC50: 59 nM (androgen receptor)

规格

别名
雄激素受体拮抗剂 1
规格或纯度
≥99%
英文名称
Androgen receptor antagonist 1
生化机理
雄激素受体拮抗剂 1 是一种可口服的完全雄激素受体(AR)拮抗剂,其 IC 50 为 59 nM。雄激素受体拮抗剂 1(化合物 6)可用于合成 PROTAC AR 降解剂,从而分别获得 24% 和 47% 的 AR 原型。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
拮抗剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
416.90

技术文档

📋 安全数据表 (SDS)

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✅ 分析证书 (COA)

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🔬 规格说明书

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高级数据

化学和物理性质
溶解性
DMSO : 100 mg/mL (239.87 mM; Need ultrasonic)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
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