Product Details
Product Name:
ARV-471 |
CAS No.:
2229711-68-4 |
Purity:
99.85% |
Supply Ability:
10g |
Release date:
2024/11/19 |
Product Introduction
Bioactivity
Name | ARV-471 |
Description | Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. It can reduce the expression of classically regulated ER target genes and inhibit the growth of ER-dependent cell lines (including those expressing ESR1 variants, such as Y537S and D538G) by degrading ER. |
In vitro | Vepdegestrant (ARV-471) is an estrogen receptor (ER) α PROTAC molecule that degrades ER in ER-positive breast cancer cell lines with a DC50 of approximately 1 nM. |
In vivo | Vepdegestrant (ARV-471) (3, 10, and 30 mpk/day, orally) demonstrated significant antitumor activity in estradiol-dependent MCF7 xenografts, with a greater than 90% reduction in ER protein; even more significant tumor growth inhibition (131% TGI) was observed in the MCF7 xenograft model, with a significant reduction in ER protein levels when combined with the CDK4/6 inhibitor palbociclib.[1] |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 100 mg/mL (138.14 mM), Sonication is recommended.
|
Keywords | oral | Inhibitor | breast cancer | PROTAC | E3 ligase | inhibit | hetero-bifunctional | ARV 471 | ubiquitylation | PROTACs | Estrogen Receptor/ERR | ARV471 | estrogen receptor | proteasome | ARV-471 |
Inhibitors Related | Kaempferol | Tamoxifen | Estradiol | Estradiol benzoate | Genistin | Cholesterol | Estriol | Chrysin | Ethisterone | Estrone |
Related Compound Libraries | Bioactive Compound Library | Drug Repurposing Compound Library | Endocrinology-Hormone Compound Library | Orally Active Compound Library | Bioactive Compounds Library Max | Anti-Cancer 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.
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Recommended supplier
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$0.00/1KG |
VIP3Y
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Henan Aochuang Chemical Co.,Ltd.
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VIP1Y
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2024-11-19 |