2. PROTAC Vitamin D Related/Nuclear Receptor Protein Tyrosine Kinase/RTK
  3. PROTACs Androgen Receptor Estrogen Receptor/ERR Src
  4. PROTAC AR Degrader-12

PROTAC AR Degrader-12 是一种高效的 PROTAC 靶向雄激素受体 (AR) 共激活因子结合位点 (AR-CBS)。PROTAC AR Degrader-12 通过泛素-蛋白酶体系统 (UPS) 途径诱导AR降解。PROTAC AR Degrader-12 通过影响DNA 复制和细胞分裂抑制肿瘤细胞生长。PROTAC AR Degrader-12 不仅能有效降解 AR，还能强效抑制 MCF-7 细胞以及多种突变或耐药乳腺癌细胞的增殖。PROTAC AR Degrader-12 通过雌激素受体α (ERα) 蛋白下调和转录活性抑制的双重机制有效阻断雌激素受体α (ERα) 信号通路。PROTAC AR Degrader-12 显著抑制 FOXA1、GREB1、SRC 和 PELP1 的 mRNA 表达。PROTAC AR Degrader-12 可用于乳腺癌的研究。
(粉色: AR 配体 (HY-179442)；蓝色: VHL 配体 (HY-112078)；黑色: 连接子)。

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PROTAC AR Degrader-12

PROTAC AR Degrader-12 Chemical Structure

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Customer Review

PROTAC AR Degrader-12 相关抗体

Top Publications Citing Use of Products

查看 PROTACs 亚型特异性产品:

查看所有亚型
von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

查看 Estrogen Receptor/ERR 亚型特异性产品:

查看所有亚型
Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

查看 Src 亚型特异性产品:

查看所有亚型
Lck Fyn Blk Fgr Hck Lyn Yes SRC-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC AR Degrader-12 is a highly efficient PROTAC targeting AR coactivator binding site (AR-CBS). PROTAC AR Degrader-12 induces AR degradation in a ubiquitin proteasome system (UPS) pathway-dependent manner. PROTAC AR Degrader-12 inhibits tumor cell growth by affecting DNA replication and cell division PROTAC AR Degrader-12 could not only effectively degrade AR, but also potently inhibit the proliferation of MCF-7 and multiple mutant or resistant BC cells. PROTAC AR Degrader-12 effectively blocked estrogen receptor α (ERα) signaling through a dual mechanism involving ERα protein downregulation and suppression of its transcriptional activity. PROTAC AR Degrader-12 significantly inhibits the mRNA expression of FOXA1, GREB1, SRC, and PELP1. PROTAC AR Degrader-12 can be used for the study of breast cancer[1]. (Pink: AR ligand (HY-179442); Blue: VHL ligand (HY-112078); Black: linker).

IC50 & Target

ERα

 

体外研究
(In Vitro)

PROTAC AR Degrader-12 (Compound 18o) 对 MCF-7 (IC50 = 0.13 μM) 和 LCC2 细胞 (IC50 = 0.54 μM) 均表现出良好的抑制活性，并对临床相关的突变体具有广谱疗效，对 MCF-7D538G (IC50 = 0.66 μM)、MCF-7Y537S (IC50 = 0.44 μM) 和 MCF-7EGFR (IC50 = 0.52 μM) 均表现出强效的亚微摩尔级抑制作用[1]。
PROTAC AR Degrader-12 (0.01-2 μM，24 小时) 能以剂量依赖的方式有效降解 MCF-7 细胞中的 AR 蛋白 (DC50 = 0.72 μM)[1]。
PROTAC AR Degrader-12 (1 μM，0-24 小时) 对 MCF-7 细胞中 AR 的降解表现出时间依赖性效应[1]。
PROTAC AR Degrader-12 (0.01-2 μM，24 小时) 导致 MCF-7 细胞中 ERα 蛋白表达呈浓度依赖性下调[1]。
PROTAC AR Degrader-12 (0.01-2 μM，12-24 小时) 显著下调 MCF-7D538G、MCF-7Y537S、MCF-7EGFR、LCC2 和 T47D 细胞中 ERα 蛋白的表达，但未能下调 PC9 细胞中 ERβ 蛋白的表达[1]。
PROTAC AR Degrader-12 (1 μM，24 小时) 通过间接机制而非直接靶向 MCF-7 细胞中 CBS 的降解来诱导 ERα 的减少[1]。
PROTAC AR Degrader-12 (0-5 μM，0-24 小时) 通过转录后降解降低 MCF-7 细胞中 AR 蛋白的表达，而 ERα 的减少则源于转录抑制[1]。
PROTAC AR Degrader-12 在 AR 过表达但 ERα 缺陷的前列腺癌细胞 LNCaP 中表现出强效的抗增殖活性 (IC50 = 0.46 μM) ，但在 AR 阴性的 MDA-MB-231 细胞中，其抗增殖活性显著降低 (IC50 > 30 μM)[1]。
PROTAC AR Degrader-12 在高温下能有效稳定 AR 蛋白，但对 ERα 蛋白的保护作用较弱，这表明PROTAC AR Degrader-12 在 LCC2 细胞中与 AR 结合，但不与 ERα 结合[1]。
PROTAC AR Degrader-12 (1 μM，24 小时) 显著抑制 MCF-7 细胞中 FOXA1、GREB1、SRC 和 PELP1 的 mRNA 表达[1]。
PROTAC AR Degrader-12 (1-10 μM，48 小时) 诱导 MCF-7 和 LCC2 细胞发生 S 期细胞周期阻滞[1]。

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

PROTAC AR Degrader-12 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 0.01 μM, 0.1 μM, 1 μM, 2 μM
Incubation Time: 0 h, 3 h, 6 h, 12 h, 18 h, 24 h
Result: Effectively and in a dose-dependent manner degraded AR protein.
Time-dependent effect on AR degradation.
Caused a concentration-dependent downregulation of ERα protein.

Real Time qPCR[1]

Cell Line: MCF-7 cells
Concentration: 0 μM, 1 μM, 5 μM
Incubation Time: 0 h, 4 h, 24 h
Result: AR mRNA expression increased significantly with increasing concentration; ERα mRNA expression was downregulated.
The expression of ERα target genes (TFF1, PGR) and AR target genes (PSA, TMPRSS2) was significantly suppressed after 24 hours.
Significantly inhibited the mRNA expression of FOXA1, GREB1, SRC, and PELP1.
体内研究
(In Vivo)

PROTAC AR Degrader-12 (Compound 18o) (5-10 μM/kg，腹腔注射，隔日一次) 可显著抑制 MCF-7 细胞和 LCC2 细胞异种移植小鼠的肿瘤生长，促进 AR 蛋白降解和 ERα 信号抑制，且不引起体重减轻或其他毒性[1]。

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

Animal Model: Balb/c nude mice (female, 4 weeks old) were subcutaneously injected with MCF-7 human breast cancer cells (5 × 106 cells)[1].
Dosage: 5 μM/kg, 10 μM/kg
Administration: I.p., once every other day
Result: At a dose of 10 μM/kg, it significantly inhibited tumor growth.
Tumor volume decreased, and Ki67 proliferation marker expression was reduced.
AR and ERα protein levels were downregulated in tumor tissue.
No significant change in body weight or significant toxicity was observed.
Animal Model: Balb/c nude mice (female, 4 weeks old) were subcutaneously injected with tamoxifen-resistant LCC2 human breast cancer cells (5 × 106 cells)[1].
Dosage: 5 μM/kg, 10 μM/kg
Administration: I.p., once every other day
Result: Tumor growth inhibition rate (TGI) reached 58% at a dose of 10 μM/kg.
Ki67 expression was decreased, and AR and ERα proteins were downregulated.
Body weight remained stable, with no signs of toxicity.
分子量

1065.33

Formula

C57H76N8O10S
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

PROTAC AR Degrader-12 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PROTAC AR Degrader-12PROTAC AR Degrader12PROTAC AR Degrader 12PROTACsAndrogen ReceptorEstrogen Receptor/ERRSrcPROTACAREndocrine ResistanceBreast CancerInhibitorinhibitorinhibit

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