计算溶液所需的质量、体积或浓度。
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。
储存与运输
避光,-20°C储存,干燥。超低温运输 。请查阅批次 COA 获取详细规格。
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。
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
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer
In Vitro
ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC 50 values of 4 nM and 5 nM, respectively. ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: VCaP cell Concentration: 1, 10, 100, and 1000 nM Incubation Time: 24 hours Result: Reduces the AR protein level and achieves the AR degradation.
In Vivo
ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours . ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice . ARD-2128 (5mg/kg; p.o.) treatment shows the C max , AUC 0-t and t 1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: SCID mice Dosage: 20 mg/kg Administration: Oral Result: Reducing the level of AR protein in mice after 24 hours. Animal Model: SCID mice Dosage: 10, 20, and 40 mg/kg Administration: P.o.; daily for 21 days Result: Inhibits tumor growth by 46, 69, and 63%, respectively. Animal Model: Male ICR Mice Dosage: 5 mg/kg Administration: P.o. (Pharmacokinetic Analysis) Result: The C max , AUC 0-t and t 1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
Form:Solid
IC50& Target:IC50: 4 nM (VCaP), 5 μM (LNCaP)
规格
规格或纯度
≥99%
英文名称
ARD-2128
生化机理
ARD-2128 是一种高效的口服生物利用型 PROTAC 雄激素受体（AR）降解剂。ARD-2128 能有效减少 AR 蛋白，抑制肿瘤组织中的 AR 调控基因，抑制肿瘤生长，且无毒性。ARD-2128 具有以下优点
储存条件
避光,-20°C储存,干燥
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
分子量
820.37
技术文档
高级数据
化学和物理性质
溶解性
DMSO : 100 mg/mL (121.90 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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