3025452-07-4
Chemical Structure
Vepdegestrant-d5
Synonym(s): ARV-471-d5 PF-07850327-d5
- CAS No.: 3025452-07-4
- Formula:C45H44D5N5O4
- Molecular Weight:728.93
InChIKey: TZZDVPMABRWKIZ-SSBBKDJISA-N
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
Biological Activity: 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].
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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. | |||||||||||||||||||||
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Vepdegestrant (Standard) | ≥98% | Vepdegestrant (Standard) is the analytical standard of Vepdegestrant (HY-138642). This product is intended for research and analytical applications. 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 half-maximal degradation concentration (DC50) of about 2 nM. | ||||||||||||||||||||
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Vepdegestrant | 99.20% | 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 half-maximal degradation concentration (DC50) of about 2 nM. | ||||||||||||||||||||
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Similarity Score 1.00
HY-138642A(Rac)-Vepdegestrant -
Similarity Score 0.88
HY-160563PROTAC ERα Degrader-8 -
Similarity Score 0.82
HY-168270PROTAC ER Degrader-11 -
Similarity Score 0.81
HY-160562PROTAC ERα Degrader-7 -
Similarity Score 0.79
HY-145071PROTAC ERα Y537S degrader-1 -
Similarity Score 0.76
HY-145073PROTAC ER Degrader-10 -
Similarity Score 0.76
HY-170340PROTAC ER Degrader-14 -
Similarity Score 0.74
HY-170336PROTAC ERα Degrader-10 -
Similarity Score 0.68
HY-164924ERD-12310A -
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