Product Details
Product Name:
ARV-471 |
CAS No.:
2229711-68-4 |
Purity:
99.85% |
Supply Ability:
10g |
Release date:
2024/11/15 |
Product Introduction
Bioactivity
名稱 | ARV-471 |
描述 | 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. |
體外活性 | 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. |
體內(nèi)活性 | 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] |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 100 mg/mL (138.14 mM), Sonication is recommended.
|
關(guān)鍵字 | oral | Inhibitor | breast cancer | PROTAC | E3 ligase | inhibit | hetero-bifunctional | ARV 471 | ubiquitylation | PROTACs | Estrogen Receptor/ERR | ARV471 | estrogen receptor | proteasome | ARV-471 |
相關(guān)產(chǎn)品 | Kaempferol | Tamoxifen | Estradiol | Estradiol benzoate | Genistin | Cholesterol | Estriol | Chrysin | Ethisterone | Estrone |
相關(guān)庫 | 經(jīng)典已知活性庫 | 藥物功能重定位化合物庫 | 內(nèi)分泌激素分子庫 | 口服活性化合物庫 | 已知活性化合物庫 | 抗癌化合物庫 |
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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