2. Vitamin D Related/Nuclear Receptor PROTAC
  3. Estrogen Receptor/ERR PROTACs
  4. (Rac)-Vepdegestrant

(Rac)-Vepdegestrant  (Synonyms: (Rac)-ARV-471)

目录号: HY-138642A
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摩尔计算器

(Rac)-Vepdegestrant 是 Vepdegestrant (HY-138642) 的异构体。Vepdegestrant ((Rac)-ARV-471) 是一种用于抵抗乳腺癌的具有口服活性的雌激素受体 PROTAC 蛋白降解剂。Vepdegestrant 是一种异双功能分子，可促进雌激素受体 α 和细胞内 E3 连接酶复合物之间的相互作用。Vepdegestrant 通过蛋白酶体导致雌激素受体的泛素化和随后的降解。Vepdegestrant 可强力降解 ER 阳性乳腺癌细胞系中的 ER，DC50 值约为 2 nM。

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(Rac)-Vepdegestrant Chemical Structure

(Rac)-Vepdegestrant Chemical Structure

CAS No. : 2229711-08-2

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(Rac)-Vepdegestrant 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

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

(Rac)-Vepdegestrant is the isomer of Vepdegestrant (HY-138642). Vepdegestrant ((R)-Lavandulol) is an orally active PROTAC estrogen receptor degrader against breast cancer. Vepdegestrant is a hetero-bifunctional molecule that facilitates the interactions between estrogen receptor alpha and an intracellular E3 ligase complex. Vepdegestrant leads to the ubiquitylation and subsequent degradation of estrogen receptors via the proteasome. Vepdegestrant robustly degrades ER in ER-positive breast cancer cell lines with a half-maximal degradation concentration (DC50) of about 2 nM[1].

分子量

723.90

Formula

C45H49N5O4
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

(Rac)-Vepdegestrant 相关分类

  • 摩尔计算器

  • 稀释计算器

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Keywords:

(Rac)-Vepdegestrant2229711-08-2(Rac)-ARV-471Estrogen Receptor/ERRPROTACsoralestrogen receptorPROTACbreast cancerhetero-bifunctionalE3 ligaseubiquitylationproteasomeInhibitorinhibitorinhibit

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