2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Androgen Receptor Apoptosis
  4. AR antagonist 15

AR antagonist 15 是一种口服有效的雄激素受体 (AR) 拮抗剂，对 ART787A 的 IC50 为 97 nM。AR antagonist 15 破坏 AR 核转位，阻碍 AR 同源二聚化，并通过与配体结合袋的竞争性结合抑制 AR 调节基因的转录。AR antagonist 15 可以显著降低前列腺特异性抗原 (PSA) 水平。AR antagonist 15 降低凋亡相关蛋白的表达诱导凋亡。AR antagonist 15 可用于前列腺癌症的研究。

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AR antagonist 15

AR antagonist 15 Chemical Structure

CAS No. : 1790308-86-9

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AR antagonist 15 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 15 is an orally active androgen receptor (AR) antagonist with the IC50 of 97 nM for ART787A. AR antagonist 15 disrupts AR nuclear translocation, hinders AR homodimerization, and suppresses transcription of AR-regulated genes by competitive binding to the ligand binding pocket. AR antagonist 15 can significantly lower the prostate-specific antigen (PSA) level. AR antagonist 15 induces apoptosis by reducing the expression of apoptosis pathway related proteins. AR antagonist 15 can be used for the research of prostate cancer[1].

体外研究
(In Vitro)

AR antagonist 15 (Compound LT16) 对雄激素受体 (AR) 及其相关突变体具有显著的拮抗活性，包括 ART787A (IC50 = 97 nM)，ARF877L (IC50 = 200 nM)，ARF877L/T787A (IC50 = 260 nM)，ARH875Y/T787A (IC50 = 200 nM)，ARW742C (IC50 = 510 nM) 和ART787G (IC50 = 555 nM)[1]。

AR antagonist 15 以剂量依赖的方式降低前列腺特异性抗原 (PSA) 的分泌水平，IC50 为 0.16 μM[1]。

AR antagonist 15 (48 小时) 促使 AR 从细胞质转移到细胞核[1]。

AR antagonist 15 (0.1-10 μM，48 小时) 可以下调 LNCaP 细胞中 AR 调节基因的 mRNA 水平，并显著降低参与凋亡途径的关键蛋白的 mRNA 水平[1]。

AR antagonist 15 (0.01-100 μM，3 天或 5 天) 显著抑制 AR 阳性细胞的增殖[1]。

AR antagonist 15 (10 μM，48 小时) 诱导 LNCaP 细胞 G0/G1 细胞周期阻滞[1]。

AR antagonist 15 (0.5-5 μM，14 天) 抑制 LNCaP 细胞的生长并减少细胞集落数量[1]。

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

AR antagonist 15 相关抗体:

Western Blot Analysis[1]

Cell Line: LNCaP cells
Concentration: 0.1 μM, 1 μM, 10 μM, Enzalutamide (Enz) (HY-70002) as a control group
Incubation Time: 48 h
Result: Reduced the level of protein TMPRSS2, FKBP5, and PSA.

RT-PCR[1]

Cell Line: LNCaP cells
Concentration: 0.1 μM, 1 μM, 10 μM
Incubation Time: 48 h
Result: Reduced the mRNA level of AR regulated genes KLK3, TMPRSS2, FKBP5, c-MYC and UBE2C.
Lowed the mRNA level of proteins related to the apoptosis pathway Cyclin A, CDK1, CDC20, and CKS2.

Cell Viability Assay[1]

Cell Line: LNCaP, LNCaP-CRPC, LNCaP-EnzR, VCaP, 22Rv1, and C4-2B cells
Concentration: 5 days for LNCaP and LNCaP-CRPC cells; 3 days for LNCaP-EnzR, VCaP, 22Rv1, and C4-2B cells
Incubation Time: 48 h
Result: Exhibited a relatively better antiproliferative effect in LNCaP (IC50 = 5.31 μM), LNCaP-CRPC (IC50 = 8.05 μM) and LNCaP-EnzR (IC50 = 5.40 μM).

Cell Cycle Analysis[1]

Cell Line: LNCaP cells
Concentration: 10 μM
Incubation Time: 48 h
Result: Caused cell cycle arrest in G0/G1.

Cell Proliferation Assay[1]

Cell Line: LNCaP cells
Concentration: 0.5 μM, 10 μM
Incubation Time: 14 days
Result: Significantly inhibited the number of cell colonies.
体内研究
(In Vivo)

AR antagonist 15 (50 mg/kg；i.g.；每日一次；持续三周) 显著减少雄性 Balb/C nude 前列腺癌小鼠肿瘤体积并降低血清 PSA 水平[1]。

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

Animal Model: 1×107 LNCaP cells injected the Balb/C nude male mice (4-6 weeks)[1]
Dosage: 50 mg/kg
Administration: Oral gavage (i.g.); once daily for three weeks
Result: Significantly reduced tumor volume and tumor weight of the cancer mice and the final tumor growth inhibition (TGI) rate was 75.63%.
Significantly inhibited the PSA level and the concentration of the PSA droped to 11.08 ng/mL. Did not cause significant changes in the weight of the mice.
分子量

346.44

Formula

C18H22N2O3S
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 15 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

AR antagonist 151790308-86-9AR antagonist15AR antagonist-15Androgen ReceptorApoptosisprostate canceranticancerPSAapoptosisInhibitorinhibitorinhibit

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