Androgen receptor-IN-2 (Synonyms: Androgen receptor-IN-2)
目录号: PL03618 纯度: ≥98%
CAS No. :2416716-62-4
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中文名称
Androgen receptor-IN-2
英文名称
Androgen receptor-IN-2
英文别名
Methanesulfonamide, N-[4-[[4-[1-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]-1-methylethyl]phenoxy]methyl]-2-pyrimidinyl]-;masofaniten;N-(4-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl)propan-2-yl)phenoxy)methyl)pyrimidin-2-yl)methanesulfonamide
Cas No.
2416716-62-4
分子式
C24H24Cl2N4O4S
分子量
535.44
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
Androgen receptor-IN-2 是一种有效的、具有口服活性的 androgen receptor 抑制剂。Androgen receptor-IN-2 对前列腺癌具有抗肿瘤活性。
生物活性
Androgen receptor-IN-2 is a potent and orally active androgen receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer.
性状
Solid
IC50 & Target[1][2]
Androgen receptor
体外研究(In Vitro)
Androgen receptor-IN-2 (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC50 of 535 nM.
Androgen receptor-IN-2 inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively).
Androgen receptor-IN-2 shows a metabolic stability in liver microsome with a t1/2 of more than 120 min, and in hepatocytes with a t1/2 of more than 360 min.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Androgen receptor-IN-2 (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors.
Androgen receptor-IN-2 (5 mg/kg, p.o., single dose, in male CD-1 mice) shows a t 1/2 of 8.1 h, C max of 2673.3 ng/mL, F (%) of 33.6.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Han-Jie Zhou, et al. Androgen receptor modulators and methods for their use. Patent. US20200123117A1.
溶解度数据
In Vitro: DMSO : 50 mg/mL (93.38 mM; Need ultrasonic and warming)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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