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Apalutamide

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Chemical Structure| 956104-40-8 同义名 : -
CAS号 : 956104-40-8
货号 : A136293
分子式 : C21H15F4N5O2S
纯度 : 98%
分子量 : 477.435
MDL号 : MFCD22380626
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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

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].
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
实验方案
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
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.