2. Vitamin D Related/Nuclear Receptor Membrane Transporter/Ion Channel
  3. Estrogen Receptor/ERR Potassium Channel
  4. ER degrader 10

ER degrader 10 (Compound 51) 是口服有效的雌激素受体 (ER) 选择性降解剂和拮抗剂，DC50 为 0.43 nM，IC50 为 0.56 nM。ER degrader 10 抑制 ER 阳性细胞的增殖，IC50 为 0-15 nM。ER degrader 10 对 hERG 通道表现出弱抑制活性，IC50 >40 μM。ER degrader 10 具有血脑屏障通透性，脑/血浆比 (Kp) 为 3.05。ER degrader 10 在小鼠模型中表现出抗肿瘤活性。

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ER degrader 10 Chemical Structure

ER degrader 10 Chemical Structure

CAS No. : 3035311-43-1

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ER degrader 10 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

ER degrader 10 (Compound 51) is a selective, orally active degrader and antagonist for estrogen receptor (ER) with a DC50 of 0.43 nM and an IC50 of 0.56 nM. ER degrader 10 inhibits the proliferation of ER-positive cells with IC50s of 0-15 nM. ER degrader 10 exhibits a weak inhibitory activity against hERG channel with an IC50 >40 μM. ER degrader 10 is blood-brain barrier penetrable with a brain/plasma ratio (Kp) of 3.05. ER degrader 10 exhibits antitumor efficacy in mice model[1].

分子量

497.60

Formula

C28H29F2NO3S
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

ER degrader 10 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:

ER degrader 103035311-43-1ER degrader10ER degrader-10Estrogen Receptor/ERRPotassium ChannelKcsAMCF-7orally activeBALB/c mouseCAMA-1BT-474MDA-MB-361Inhibitorinhibitorinhibit

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