2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. Bexirestrant

Bexirestrant 是一种具有口服活性的 ER-α 降解剂。Bexirestrant 可用于抗雌激素、抗肿瘤的研究。

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Bexirestrant Chemical Structure

Bexirestrant Chemical Structure

CAS No. : 2505067-70-7

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Bexirestrant 相关抗体

Top Publications Citing Use of Products

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

Bexirestrant is an orally active ER-α degrader. Bexirestrant can be used for the research of antiestrogen, antineoplastic[1][2].

体外研究
(In Vitro)

Bexirestrant (compound Formula Ia) inhibits the growth of wild type (WT), Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 6.0, 2.2 nM, respectively[1].
Bexirestrant induces the ER-α degradation in WT, Y537S and D538G mutated MCF-7 cells with IC50s of 0.3. 19.6, 12.7 nM, respectively[1].
Bexirestrant shows 16.3% ER-α remaining in WT MCF-7 cells at concentration of 1 nM[1].

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

Bexirestrant 相关抗体:
体内研究
(In Vivo)

Bexirestrant (50mg/kg; p.o.; 28 days) shows a good efficacy in an MCF-Y537S xenograft[1]. Pharmacokinetic parameters in rat at 50 mg/kg p.o. dose[1]：

Tmax (h) Cmax (ng/mL) AUClast (hr× ng/mL) AUCinf_obs (hr×ng/mL) T1/2 (h)
4.00 343 7582 9804 26

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

Animal Model: Female athymic nude mice harboring subcutaneous MCF7-Y537S xenograft[1]
Dosage: 50mg/kg
Administration: p.o. for 28 days
Result: Showed 56% tumor growth inhibition compared to vehicle group after 28 days.
分子量

477.52

Formula

C29H26F3NO2
CAS 号
Unlabeled CAS

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

Bexirestrant 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:

Bexirestrant2505067-70-7Estrogen Receptor/ERRMCF-7 cellsY537S mutatD538G mutatcancerantiestrogenInhibitorinhibitorinhibit

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目录号：
HY-145556
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