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/ 雄激素受体 / Apalutamide

Apalutamide {[allProObj[0].p_purity_real_show]}

货号：A136293

ARN-509 can compeitively and selectively inhibit androgen receptor with IC50 value of 16 nM.

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Apalutamide 化学结构 CAS号：956104-40-8
Apalutamide 化学结构
CAS号：956104-40-8
Apalutamide 3D分子结构
CAS号：956104-40-8
Apalutamide 化学结构 CAS号：956104-40-8
Apalutamide 3D分子结构 CAS号：956104-40-8
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Apalutamide 纯度/质量文件 产品仅供科研

货号：A136293 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Androgen Receptor ↓ 其他靶点 纯度
Cyproterone acetate ++++

Androgen Receptor, IC50: 7.1 nM

 		98%
Apalutamide +++

Androgen Receptor, IC50: 16 nM

 		98%
AZD3514 +

Androgen Receptor, Ki: 2.2 μM

 		98%
Darolutamide ++++

Androgen receptor, Ki: 11 nM

 		98%
Flutamide +++

Androgen Receptor, Ki: 55 nM

 		98%
Galeterone ++

Androgen Receptor, IC50: 384 nM

 		98%
Enzalutamide +++

Androgen Receptor, IC50: 36 nM

 		98%
Megestrol ✔ 98%
Bicalutamide ++

Androgen Receptor, IC50: 0.16 μM

 		99%
EPI-001 +

Androgen Receptor, IC50: ~6 μM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Apalutamide 生物活性

靶点

  • Androgen Receptor

    Androgen Receptor, IC50:16 nM
描述 The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. ARN-509 is a competitive AR inhibitor (IC50=16 nM) which is fully antagonistic to AR overexpression, a common and important feature of castration-resistant prostate cancer (CRPC). In castration-resistant LNCaP/AR cells, ARN-509 (< 10 μM; 3d) antagonized androgen-mediated induction or repression of mRNA expression-levels for 13 endogenous genes including PSA and TMPRSS2, and ARN-509 (< 10 μM) also antagonized the proliferative effect of R1881 (30pM). Following 17 days of treatment with ARN-509 (10 mg/kg/day) in a model of castration-resistant prostate cancer, androgen-driven luciferase reporter-gene activity was consistently reduced compared to vehicle, indicating AR inhibition by ARN-509 in vivo. In castrate mice bearing LNCaP/AR (cs) xenograft tumors, 8/10 ARN-509-treated (10 mg/kg/day) tumors regressed by >50% (volume) on day 28 [8].

Apalutamide 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
LNCAP cells Proliferation assay 3 days Antiproliferative activity against human LNCAP cells after 3 days, IC50=0.174 μM 26046313
PSN1 cells Cytotoxicity assay 96 h Cytotoxicity against human PSN1 cells after 96 hrs by ATP-lite luminescence assay, IC50=0.06 μM 22247788
PSN1 cells 30 nM Function assay 24 h Induction of cell cycle arrest in human PSN1 cells assessed as accumulation at G2/M phase cells at 30 nM after 24 hrs by flow cytometry 22247788

Apalutamide 动物研究

Dose Mice: 10 mg/kg - 100 mg/kg[3] (p.o.), 2 mg/kg[4] (p.o. or i.v.); 1 mg/kg[5] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Mice[4] Rats[6]
Dose 2 mg/kg 10 mg/kg
Administration p.o. or i.v. p.o.
F 126% (p.o.)
Vd 2.51 L/kg (i.v.)
T1/2 24.7 h 7.4 ± 0.4 h
Tmax 4.00 h (p.o.) 3.5 ± 0.6 h
CL 1.17 mL/min/kg (i.v.)
Cmax 855 ng/ml (p.o.) 946 ± 43 ng/ml
MRT 10.7 ± 0.5 h
AUC0→∞ 35,941 ng·h/ml (p.o.)
28,463 ng·h/ml (i.v.) 		14,752 ± 1997 h·ng/ml

Apalutamide 参考文献

[1]Clegg NJ, Wongvipat J, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503.

[2]Hallur G, Purra BR, et al. Validation of an LC-ESI-MS/MS method for the determination of apalutamide, a novel non-steroidal anti-androgen in mice plasma and its application to a pharmacokinetic study in mice. J Pharm Biomed Anal. 2018 May 10;153:260-266.

[3]Saini NK, Sulochana SP, et al. A novel dried blood spot LC-MS/MS method for the quantification of apalutamide in mouse whole blood: Application to pharmacokinetic study in mice. Biomed Chromatogr. 2018 Nov;32(11):e4344.

[4]Pang X, Wang Y, et al. Design, synthesis, and biological evaluation of deuterated apalutamide with improved pharmacokinetic profiles. Bioorg Med Chem Lett. 2017 Jun 15;27(12):2803-2806.

[5]Shukla GC, Plaga AR, Shankar E, Gupta S. Androgen receptor-related diseases: what do we know? Andrology. 2016 May;4(3):366-81. doi: 10.1111/andr.12167. Epub 2016 Mar 16. PMID: 26991422.

[6]Clegg NJ, Wongvipat J, Joseph JD, Tran C, Ouk S, Dilhas A, Chen Y, Grillot K, Bischoff ED, Cai L, Aparicio A, Dorow S, Arora V, Shao G, Qian J, Zhao H, Yang G, Cao C, Sensintaffar J, Wasielewska T, Herbert MR, Bonnefous C, Darimont B, Scher HI, Smith-Jones P, Klang M, Smith ND, De Stanchina E, Wu N, Ouerfelli O, Rix PJ, Heyman RA, Jung ME, Sawyers CL, Hager JH. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012 Mar 15;72(6):1494-503. doi: 10.1158/0008-5472.CAN-11-3948. Epub 2012 Jan 20. PMID: 22266222; PMCID: PMC3306502.

Apalutamide 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.09mL

0.42mL

0.21mL

10.47mL

2.09mL

1.05mL

20.95mL

4.19mL

2.09mL

Apalutamide 技术信息

CAS号956104-40-8
分子式C21H15F4N5O2S
分子量 477.435
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature
溶解度
动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 4 mg/mL clear

PO 0.5% CMC-Na 60 mg/mL suspension

Tags: Apalutamide | Androgen Receptor | AmBeed-信号通路专用抑制剂 | Apalutamide 纯度/质量文件 | Apalutamide 亚型比较 | Apalutamide 生物活性 | Apalutamide 细胞研究 | Apalutamide 动物研究 | Apalutamide 参考文献 | Apalutamide 实验方案 | Apalutamide 技术信息

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