VPC-14449

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VPC-14449  纯度: 98.89%

VPC-14449 是一种有效和选择性的雄激素受体 DNA 结合结构域 (AR-DBD) 抑制剂,对全长人 AR 的 IC50 值为 0.34 μM。VPC-14449 可降低全长 AR 以及 AR 变体与染色质相互作用的能力。VPC-14449 可用于前列腺癌的研究。

VPC-14449

VPC-14449 Chemical Structure

CAS No. : 1621375-32-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥3300 In-stock
5 mg ¥3000 In-stock
10 mg ¥4800 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

VPC-14449 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Anti-Cancer Compound Library
  • Transcription Factor Targeted Library

生物活性

VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer[1][2].

IC50 & Target

IC50: 0.34 μM (AR-DBD)[1]

体外研究
(In Vitro)

VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells[2].
VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells (IC50=0.34 μM) without affecting AR protein expression[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells
Concentration: 0.01, 0.1, 10, 100 μM
Incubation Time: 24 hours
Result: Suppressed the growth of every tested cell line.

Western Blot Analysis[2]

Cell Line: LNCaP, C4-2, MR49F, and 22Rv1 cells
Concentration: 0.01, 0.1, 10, 100 μM
Incubation Time: 24 hours
Result: Inhibited endogenous AR transactivation in LNCaP, C4-2 and MR49F cells stimulated with the synthetic androgen R1881.

体内研究
(In Vivo)

VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice (Harlan Sprague-Dawley; 25-31 g; 6-8 weeks) were subcutaneously inoculated with LNCaP cells and castrated[1]
Dosage: 100 mg/kg
Administration: I.p. twice daily for 4 weeks
Result: Suppressed LNCaP tumor volume and blocked serum PSA production.

分子量

394.09

Formula

C10H10Br2N4OS

CAS 号

1621375-32-3

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 : 125 mg/mL (317.19 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5375 mL 12.6875 mL 25.3749 mL
5 mM 0.5075 mL 2.5375 mL 5.0750 mL
10 mM 0.2537 mL 1.2687 mL 2.5375 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 (5.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.28 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 (5.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.28 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 (5.28 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.28 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Dalal K, et, al. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. J Biol Chem. 2014 Sep 19;289(38):26417-26429.

    [2]. Dalal K, et, al. Bypassing Drug Resistance Mechanisms of Prostate Cancer with Small Molecules that Target Androgen Receptor-Chromatin Interactions. Mol Cancer Ther. 2017 Oct;16(10):2281-2291.

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