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

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

Cat. No.: HY-138642A
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(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.

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(Rac)-Vepdegestrant Chemical Structure

(Rac)-Vepdegestrant Chemical Structure

CAS No. : 2229711-08-2

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Other Forms of (Rac)-Vepdegestrant:

(Rac)-Vepdegestrant Related Antibodies

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Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

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Description

(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].

Molecular Weight

723.90

Formula

C45H49N5O4
CAS No.
SMILES

O=C(C(N(CC1=C2C=CC(N3CCN(CC4CCN(C5=CC=C([C@H]6[C@@H](C7=CC=CC=C7)CCC8=C6C=CC(O)=C8)C=C5)CC4)CC3)=C1)C2=O)CC9)NC9=O
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(Rac)-Vepdegestrant Related Classifications

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  • 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:

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

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