Vepdegestrant-d5

Vepdegestrant-d5 (ARV-471-d5) is the deuterium labeled Vepdegestrant (HY-138642) . Vepdegestrant (ARV-471) 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 DC50 of about 2 nM[1].

Product Specifications

CAS Number

[3025452-07-4]

Product Name Alternative

ARV-471-d5

UNSPSC

12352005

Target

Isotope-Labeled Compounds

Related Pathways

Others

Field of Research

Cancer

Smiles

O=C1NC([C@@H](N(C2=O)CC3=C2C=CC(N(CC4)CCN4CC(CC5)CCN5C(C=C6)=CC=C6[C@H]7[C@@H](C8=C([2H])C([2H])=C([2H])C([2H])=C8[2H])CCC9=C7C=CC(O)=C9)=C3)CC1)=O

Molecular Formula

C45H44D5N5O4

Molecular Weight

728.93

References & Citations

[1]Lin X, et al. Targeting estrogen receptor α for degradation with PROTACs: A promising approach to overcome endocrine resistance. Eur J Med Chem. 2020;206:112689.