rel-Vepdegestrant
(Rac)-Vepdegestrant is the relative configuration of Vepdegestrant (HY-138642). Vepdegestrant 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.
(Pink: ERα Target protein ligand; Blue: Cereblon ligand (HY-138793); Black: linker).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2614417-52-4
- 分子式: C45H49N5O4
- 分子量:723.90
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
2.7 nM
Compound: 7; ARV-471
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Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo reagent based luminescence analysis
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by CellTiter-Glo reagent based luminescence analysis
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[PMID: 39610216] |
| MCF7 | IC50 |
133 nM
Compound: 7; ARV-471
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Antiproliferative activity against human MCF7 cells harboring ER-alpha Y537S mutant assessed as inhibition of cell growth
Antiproliferative activity against human MCF7 cells harboring ER-alpha Y537S mutant assessed as inhibition of cell growth
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[PMID: 39610216] |
化学情報
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CAS 番号 2614417-52-4
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分子量 723.90
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分子式 C45H49N5O4
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SMILES
OC1=CC=C([C@@H](C2=CC=C(N3CCC(CC3)CN4CCN(C5=CC=C(C(N([C@@H]6C(NC(CC6)=O)=O)C7)=O)C7=C5)CC4)C=C2)[C@@H](C8=CC=CC=C8)CC9)C9=C1
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別名
rel-ARV-471; rel-PF-07850327
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
rel-Vepdegestrant 関連分類
HY-138642B 関連分類
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