2. PROTAC Vitamin D Related/Nuclear Receptor Apoptosis
  3. PROTACs Estrogen Receptor/ERR Apoptosis
  4. PROTAC ERα Degrader-12

PROTAC ERα Degrader-12 是一种强效且高选择性的 ERα PROTAC 降解剂。PROTAC ERα Degrader-12 对多种野生或突变型 ERα 的乳腺癌细胞系具有抗增殖作用，阻滞细胞周期，诱导细胞凋亡 (apoptosis)。PROTAC ERα Degrader-12 具有出色的抗肿瘤活性。PROTAC ERα Degrader-12 可用于乳腺癌的研究。(粉色：ER ligand-11 (HY-174475)；蓝色：VHL ligand (HY-112078)；黑色：连接子 (HY-W088749)；VHL ligand + Linker ( HY-W998310))。

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PROTAC ERα Degrader-12

PROTAC ERα Degrader-12 Chemical Structure

1.  客户无需承担相应的运输费用。

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Customer Review

PROTAC ERα 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC ERα Degrader-12 is a potent and selective Erα PROTAC degrader. PROTAC ERα Degrader-12 has antiproliferative effects in multiple breast cancer cell lines with wild-type or mutant ERα. PROTAC ERα Degrader-12 can halt the cell cycle and induce cell apoptosis. PROTAC ERα Degrader-12 exhibits excellent antitumor and ERα degradation activity. PROTAC ERα Degrader-12 can be used for research on breast cancer. (Pink: ER ligand-11 (HY-174475); Blue: VHL ligand (HY-112078); Black: Linker (HY-W088749); VHL ligand + Linker ( HY-W998310))[1].

IC50 & Target[1]

ERα

 

VHL

 

体外研究
(In Vitro)

PROTAC ERα Degrader-12 (Compound CP03) (0.1-10 μM, 24 h) 在 MCF-7 细胞中显示出显著的降解活性，其 DC50 值为 1.02 μM[1]。
PROTAC ERα Degrader-12 (0.01-100 μM, 24 h) 在 MCF-7 细胞中具备显著的抗肿瘤活性 (IC50 = 0.17 μM)[1]。
PROTAC ERα Degrader-12 在人肝微粒体和血浆中表现出显著的稳定性，其血浆蛋白结合率为 97.8%[1]。
PROTAC ERα Degrader-12 (1-5 μM, 48 h) 在 MCF-7 细胞中可阻滞细胞周期 (G1)，并诱导细胞出现大量死亡和损伤[1]。

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

PROTAC ERα Degrader-12 相关抗体:

Western Blot Analysis[1]

Cell Line: MCF-7, MDA-MB-321, MCF-7Y537S, MCF-7D538G, MCF-7EGFR, and LCC-2 cell lines
Concentration: 0.1, 0.2, 1, 2, 5, 10 μM
Incubation Time: 24 h
Result: Effectively induced ERα degradation in a dose-dependent manner in MCF-7 cells.
Efficiently reduced the ErαMUT levels in both the MCF-7Y537S and MCF-7D538G cell lines with DC50 values of 0.83 and 0.55 μM, respectively.
Showed high degradation potency for ERα in MCF-7EGFR and LCC-2 cell lines, with DC50 values of 0.13 and 1.40 μM, respectively.

Western Blot Analysis[1]

Cell Line: MCF-7
Concentration: 2 μM
Incubation Time: 24 h
Result: Was markedly suppressed in the presence of CoA-1 or CoA-2.

Cell Viability Assay[1]

Cell Line: MCF-7, MDA-MB-321, MCF-7Y537S, MCF-7D538G, MCF-7EGFR, and LCC-2 cell lines
Concentration: 0.01, 0.1, 1, 10, 100 μM
Incubation Time: 24 h
Result: Had no notable inhibitory influence on cell growth in the ER-negative cell line MDA-MB-231 at concentrations exceeding 100 μM.
Exhibited excellent antiproliferative activity in MCF-7 Y537S , MCF-7D538G , and MCF-7EGFR, with IC50 values that were 10.3-, 19.4-, and 58.0-fold higher than those of Ful, respectively.
Displayed enhanced antiproliferative efficacy against Tamoxifen (HY-13757A)-resistant LCC-2 cells, with an IC50 value that was 8.04-fold higher than that of Fulvestrant (HY-13636).

RT-PCR[1]

Cell Line: MCF-7
Concentration: 0.1, 1 μM
Incubation Time: 24 h
Result: Had no discernible impact on the mRNA of ERα expression.

Apoptosis Analysis[1]

Cell Line: MCF-7, MDA-MB-321, MCF-7Y537S, MCF-7D538G, MCF-7EGFR, and LCC-2 cell lines
Concentration: 1, 5 μM
Incubation Time: 48 h
Result: Induced substantial cellular death and damage in a concentration-dependent manner.
Effectively halted the cell cycle progression in the G1 phase.
体内研究
(In Vivo)

PROTAC ERα Degrader-12 (Compound CP03) (1-4 mg/kg, i.p., 每隔一天, 共 26 或 33 天) 在小鼠 MCF-7 和 LCC-2 肿瘤异种移植模型中具有显著的抗肿瘤效果[1]。

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

Animal Model: MCF-7 and LCC-2 tumor xenograft models established in female BALB/c nude mice (15-18 g, 5 weeks old) [1]
Dosage: 1, 2, 4 mg/kg
Administration: Intraperitoneal injection (i.p.), every other day, for 26 or 33 days.
Result: Showed significant tumor growth inhibitory activity at 2 mg/kg.
Had no significant host toxicity as monitored by changes in the body weight.
Almost completely inhibited tumor growth on day 33 at a dose of 2 or 4 mg/kg.
Effectively induced significant degradation of ERα with 2 mg/kg.
分子量

930.34

Formula

C53H83N7O5S
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 ERα Degrader-12 相关分类

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  • 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 ERα Degrader-12PROTAC ERα Degrader12PROTAC ERα Degrader 12PROTACsEstrogen Receptor/ERRApoptosisBreast cancerErαPROTACMCF-7LCC-2Inhibitorinhibitorinhibit

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