| Name | Vepdegestrant |
| 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 | 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 | 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 Compound Library | Anti-Cancer Drug Library | Anti-Cancer Active Compound Library |
United States
