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ARV-471

Catalog No. T39710Cas No. 2229711-68-4
Alias Vepdegestrant

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.

ARV-471

ARV-471

Purity: 100%
Catalog No. T39710Alias VepdegestrantCas No. 2229711-68-4
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.
Pack SizePriceAvailabilityQuantity
1 mg$265In Stock
5 mg$657In Stock
10 mg$935In Stock
25 mg$1,390In Stock
50 mg$1,890In Stock
1 mL x 10 mM (in DMSO)$896In Stock
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Purity:100%
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Product Introduction

Bioactivity
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]
AliasVepdegestrant
Chemical Properties
Molecular Weight723.9
FormulaC45H49N5O4
Cas No.2229711-68-4
Storage & Solubility Information
StoragePowder: -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.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.3814 mL6.9070 mL13.8141 mL69.0703 mL
5 mM0.2763 mL1.3814 mL2.7628 mL13.8141 mL
10 mM0.1381 mL0.6907 mL1.3814 mL6.9070 mL
20 mM0.0691 mL0.3454 mL0.6907 mL3.4535 mL
50 mM0.0276 mL0.1381 mL0.2763 mL1.3814 mL
100 mM0.0138 mL0.0691 mL0.1381 mL0.6907 mL

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