2. Vitamin D Related/Nuclear Receptor
  3. Androgen Receptor
  4. AR antagonist 17

AR antagonist 17 是一种具有选择性、口服活性、不易透过血脑屏障的雄激素受体 (AR) 拮抗剂 (IC50 = 0.010 μM) ，可有效阻断 AR 二聚化和核转位，并在多种去势抵抗性前列腺癌 (CRPC) 细胞中表现出强效作用。AR antagonist 17 对多种耐药性 AR 突变体表现出优异的疗效。AR antagonist 17 在 LNCaP 异种移植模型中抑制肿瘤生长，且无明显毒性。AR antagonist 17 可用于去势抵抗性前列腺癌 (CRPC) 的研究。

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AR antagonist 17

AR antagonist 17 Chemical Structure

CAS No. : 3064715-04-1

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AR antagonist 17 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC)[1].

体外研究
(In Vitro)

AR antagonist 17 (Compound C13) (72-120 小时) 对 AR 阳性 PCa 细胞系 (LNCaP (IC50 = 1.02 μM), C4−2B (IC50 = 3.86 μM), 22RV1 (IC50=8.45 μM), 和 VCaP (IC50 = 5.72 μM)) 表现出优异的 AR 拮抗活性和抗增殖作用，同时对正常细胞系 3T3 和 Ges-1 (IC50 > 20 μM) 具有低毒性[1]。
AR antagonist 17 (0.2-2 μM，2 周) 可完全抑制 LNCaP 细胞的克隆性增殖[1]。
AR antagonist 17 (0.02-2 μM，48 小时) 剂量依赖性地抑制双氢睾酮 (DHT) 诱导的前列腺特异性抗原 (PSA) 转录水平，并显著抑制 LNCaP 细胞中两个 AR 调控的下游基因 FKBP5 和 TMPRSS2 的 mRNA 水平[1]。
AR antagonist 17 (0.1-10 μM，24 小时) 剂量依赖性地抑制内源性 PSA 蛋白表达，但对 LNCaP 细胞中的 AR 蛋白表达无显著影响[1]。
AR antagonist 17 (0.1-10 μM，4 小时) 剂量依赖性地抑制 DHT 诱导的 AR 二聚化，并在 293T 细胞中以 10 μM 的浓度完全阻断该过程[1]。
AR antagonist 17 (10 μM，8 小时) 可使 AR 主要停留在细胞质中，并有效阻止 LNCaP 细胞中的 AR核易位[1]。
AR antagonist 17 (24 小时) 对临床上常见的 AR 耐药突变 (ARF877L/T878A (IC50 = 0.35 μM), ARW742C (IC50 = 0.50 μM), ARF877L (IC50 = 0.070 μM)) 表现出优异的拮抗活性[1]。
AR antagonist 17 (2 μM，48 小时) 显著抑制 LNCaP 细胞中 8 种临床相关的 PCa 复发标志物：KLK3 (编码 PSA) 、TMPRSS2、KLK2、NKX3.1、SLC45A3、PMEPA1、TARP 和 TM4SF1，以及癌症相关过程、凋亡调节因子 STK39、HERC3 和 GRIN3A[1]。
AR antagonist 17 (2 μM，48 小时) 显著抑制 LNCaP 细胞中与 DNA 生物合成和修复相关的泛癌相关生物标志物的表达，包括 EXO1、CYP11A1、PGC、RRM2 和 FAM111B[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

AR antagonist 17 相关抗体:

Cell Proliferation Assay[1]

Cell Line: LNCaP cells
Concentration: 0.2 μM, 2 μM
Incubation Time: 2 week
Result: Inhibited clonal proliferation at a concentration of 2.0 μM, showing better inhibitory activity against clonal proliferation than Enz 0.2 μM.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.1 Μm, 1 μM, 10 μM
Incubation Time: 24 h
Result: Inhibited endogenous PSA protein expression but had no significant effect on AR protein expression in LNCaP cells.

RT-PCR[1]

Cell Line: LNCaP cells
Concentration: 0.02 μM, 0.2 μM, 2 μM
Incubation Time: 48 h
Result: Suppressed the DHT-induced transcriptional levels of prostate-specific antigen (PSA), and remarkably suppressed mRNA levels of two AR-regulated downstream genes, FKBP5 and TMPRSS2.

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 10 μM
Incubation Time: 8 h
Result: Effectively inhibited DHT-induced AR nuclear translocation; AR mainly remains in the cytoplasm.

RT-PCR[1]

Cell Line: LNCaP cells
Concentration: 2 μM
Incubation Time: 48 h
Result: Significantly suppressed eight clinically relevant PCa recurrence markers: KLK3 (encoding PSA), TMPRSS2, KLK2, NKX3.1, SLC45A3, PMEPA1, TARP, and TM4SF1, alongside cancer-related processes, apoptosis regulators STK39, HERC3, and GRIN3A in LNCaP cells.
Significantly inhibited the expression of the pan-cancer-related biomarkers for DNA biosynthesis and repair, including EXO1, CYP11A1, PGC, RRM2, and FAM111B in LNCaP cells.
体内研究
(In Vivo)

AR antagonist 17 (5 mg/kg，经口灌胃，2-8 小时) 在 SD 大鼠中具有较低的血脑屏障通透性，可能具有更好的安全性并减少中枢神经系统相关的副作用[1]。
AR antagonist 17 (40 mg/kg，经口灌胃，每日两次，共 32 天) 对 CB17 SCID 小鼠在整个治疗期间表现出显著的肿瘤生长抑制作用，并且在实验期间不会引起明显的体重减轻或其他毒性迹象[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SD Rats[1]
Dosage: 5.0 mg/kg
Administration: Oral gavage
Result: Had low blood-brain barrier permeability in SD Rats.
Animal Model: LNCaP cells (1 × 107) were implanted subcutaneously into the right flanks of the 6-week-old male CB17 SCID mice[1].
Dosage: 40 mg/kg
Administration: Oral gavage, twice daily for 32 days
Result: The tumor growth inhibition (TGI) of AR antagonist 17 was 123.41%.
Exhibited good tolerance and did not induce significant body weight loss or other signs of toxicity during the experiment.
分子量

499.53

Formula

C21H20F3N3O4S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

AR antagonist 17 相关分类

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Keywords:

AR antagonist 173064715-04-1AR antagonist17AR antagonist-17Androgen ReceptorProstate CancerPCaCastration-Resistant Prostate CancerCRPCARAR Signaling PathwayInhibitorinhibitorinhibit

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