VPC-14449|1621375-32-3|-陌孚医药/Medlife

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VPC-14449

目录号: PL02304 纯度: ≥98%

CAS No. :1621375-32-3

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中文名称	VPC-14449
英文名称	VPC-14449
英文别名	VPC-14449;4-(4-(2,4-dibromo-1H-imidazol-1-yl)thiazol-2-yl)morpholine;4-[4-(2,4-dibromoimidazol-1-yl)-1,3-thiazol-2-yl]morpholine
Cas No.	1621375-32-3
分子式	C₁₀H₁₀Br₂N₄Os
分子量	394.09
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	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。
生物活性	VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC 50 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.
性状	Solid
IC50 & Target[1][2]	IC50: 0.34 μM (AR-DBD)
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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay
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. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
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
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.

溶解度数据	In Vitro: DMSO : 125 mg/mL (317.19 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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