2. Vitamin D Related/Nuclear Receptor Immunology/Inflammation Apoptosis
  3. Estrogen Receptor/ERR Aryl Hydrocarbon Receptor Apoptosis MDM-2/p53
  4. X15695

X15695 是一种具有选择性且口服有效的雌激素受体 (ERα) 降解剂。X15695 是一种芳香烃受体 (AHR) 配体。X15695 能使 AHR 与 ERα 形成复合物，促进其通过蛋白酶体进行降解。X15695 能抑制乳腺癌细胞的增殖，促进细胞周期停滞，并诱导细胞凋亡 (apoptosis)。X15695 可用于乳腺癌的研究。

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X15695

X15695 Chemical Structure

CAS No. : 353258-25-0

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X15695 相关抗体

Top Publications Citing Use of Products

查看 Estrogen Receptor/ERR 亚型特异性产品:

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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

X15695 is selective and orally active estrogen receptor (ERα) degrader. X15695 is an aryl hydrocarbon receptor (AHR) ligand. X15695 enables AHR to form a complex with the ERα, promoting its proteasomal degradation. X15695 inhibits the breast cancer cells proliferation, promotes cell cycle block and induces apoptosis. X15695 can be used for the study of breast cancer[1][2].

IC50 & Target[1]

ERα

 

体外研究
(In Vitro)

X15695 能抑制 MCF-7、MC7 和 MC7 细胞的增殖，其 IC50 值分别为 0.7、74.42 和 0.38 nM，在 E2 存在的情况下，其 IC50 值分别为 10.28、48.01 和 10.78 nM[1]。 X15695 在 AHR 活性被 CH223191 (HY-12684) 抑制时，仍能抑制 MCF-7 细胞的克隆生长[1]。 X15695 (1-10 μM，7 天) 抑制来自患者来源的异种移植肿瘤组织 (PDxO) 的器官状体的生长[1]。 X15695 (1 μM，48 小时) 通过激活野生型 p53 并破坏突变型 p53 的致瘤功能增强作用，分别阻滞 MCF-7 细胞、T47D 细胞、LNCaP 细胞和 LAPC-4 细胞周期，并且诱导了细胞凋亡[2]。

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

X15695 相关抗体:

Apoptosis Analysis[2]

Cell Line: MCF-7 cells, T47D cells, LNCaP cells and LAPC-4 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced apoptosis in ER+ breast cancer cells, and the apoptotic effect was more significant in wild-type p53 cells.

Cell Cycle Analysis[2]

Cell Line: MCF-7 cells, T47D cells, LNCaP cells and LAPC-4 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Significantly arrested the cells in the G1 phase in MCF-7 cells and G2/M phase in T47D cells.
Induced G1/S phase arrest in the LNCaP cells and a G2/M arrest in the LAPC-4 cells.

Western Blot Analysis[2]

Cell Line: MCF-7 cells and T47D cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Significantly increase the level of p53 protein in MCF-7 cells.
Had no significant impact in T47D cells.
体内研究
(In Vivo)

X15695 (15-30 mg/kg, 灌胃, 每日一次共 16-42 天) 在小鼠模型中有效地抑制了乳腺肿瘤的生长，但对前列腺肿瘤的生长效果较差[2]。

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

Animal Model: MCF-7 and LAPC-4 cells induced xenograft model established in 6–7weeks old female(for MCF-7 cells) and male (forLAPC-4cells) athymic nude-Foxn1nu mice (Envigo 6901M)[2
Dosage: 30 mg/kg for MCF-7 model; 15 and 30 mg/kg for LAPC-4 model
Administration: Oal gavage (i.g), once daily for 16 days (MCF-7 model) or 42 days (LAPC-4 model)
Result: Significantly inhibits tumor growth, without weight loss or other toxic signs in MCF-7 model.
Downregulated ERα and upregulated p53 in tumor tissue.
Inhibited the growth of prostate tumors (30 mg/kg), but the effect was relatively weak.
分子量

314.67

Formula

C14H7ClF4N2
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

X15695 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:

X15695353258-25-0X 15695X-15695Estrogen Receptor/ERRAryl Hydrocarbon ReceptorApoptosisMDM-2/p53AhRMCF-7 cellsT47D cellsLNCaP cellsLAPC-4 cellsPatient-derived xenograft tumoursmice modelInhibitorinhibitorinhibit

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目录号：
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