Product Details
| Product Name:
Vepdegestrant |
CAS No.:
2229711-68-4 |
| Purity:
99.93% |
Supply Ability:
10g |
| Release date:
2026/06/15 |
Product Introduction
Bioactivity
| Name | Vepdegestrant |
| Description | Vepdegestrant (ARV-471) is a selective and highly potent estrogen receptor (ER, ESR1) PROTAC degrader with strong degrading activity against the ER protein. By directly degrading the ER protein rather than merely antagonizing its activity, vepdegestrant effectively inhibits the ER signaling pathway and demonstrates significant antitumor activity in ER-positive (ER?) breast cancer, with a DC50 value of approximately 2 nM. It is particularly effective against tumors harboring ESR1 mutations. |
| In vitro | Methods: MCF7 cells were treated with 100 nM Vepdegestrant for 0–24 hours, followed by Western blot analysis to detect ER expression.
Results: ER degradation occurred rapidly, with >80% ER degraded within 4 hours. [1] |
| In vivo | Methods: MCF7 breast cancer cells were orthotopically transplanted into mice. Vepdegestrant (10 mg/kg/day) was administered orally once daily for 3 consecutive days. The mice were euthanized 18 hours after dosing, and tumor tissue was collected for Western blot analysis of ER levels.
Results: Vepdegestrant caused a ≥90% reduction in intratumoral ER levels. [1]
Methods: MCF7, T47D, and other ER+ breast cancer cells were treated with Vepdegestrant (ARV-471) and stimulated with 10 ng/mL IFN-γ for 24 hours; cell surface MHC-I expression was detected by flow cytometry.
Results: As a novel selective estrogen receptor degrader (SERD), vepdegestrant significantly reversed the inhibitory effect of estrogen on IFN-γ-induced MHC-I expression and effectively upregulated the levels of key antigen-presenting molecules.[2] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween-80+45% Saline : 3.3 mg/mL (4.56 mM), Sonication is recommended.
DMSO : 15.28 mg/mL (21.11 mM), Sonication is recommended.
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| Keywords | ubiquitylation | proteasome | PROTACs | PROTAC | oral | Inhibitor | inhibit | hetero-bifunctional | EstrogenReceptor | Estrogen Receptor/ERR | estrogen receptor | ERR | E3 ligase | breast cancer | ARV-471 | ARV471 | ARV 471 |
| Inhibitors Related | Tamoxifen | Estradiol | 2-Ethylhexyl trans-4-methoxycinnamate | Diisopropyl phthalate | Estradiol benzoate | Bisphenol B | Mequinol | Phthalic acid | Chlorothalonil | Ethisterone | Tamoxifen Citrate | Cholesterol |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | ReFRAME Related Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
Recommended supplier
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Suppliers |
Update time |
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Anhui Ruihan Technology Co., Ltd
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2023-08-21 |
United States