elacestrant (MedChemExpress)
Structured Review

Elacestrant, supplied by MedChemExpress, used in various techniques. Bioz Stars score: 94/100, based on 16 PubMed citations. ZERO BIAS - scores, article reviews, protocol conditions and more
https://www.bioz.com/result/elacestrant/product/MedChemExpress
Average 94 stars, based on 16 article reviews
Images
1) Product Images from "Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer"
Article Title: Mutant p53 binds and controls estrogen receptor activity to drive endocrine resistance in ovarian cancer
Journal: Genes & development
doi: 10.1101/gad.352953.125
Figure Legend Snippet: ( A ) IC 50 analysis in PEO1 cells transfected with non-targeting control (siNC) or sip53 for 24 hours and then plated in equal number and then treated with indicated doses of Fulvestrant for 72 hours. n = 6 biological replicates. p53 silencing was assessed by Western blot. ( B ) Colony forming assay for PEO1 cells transfected with siNC or sip53 and then treated with 10 μM Fulvestrant for 24 hours, followed by plating of equal cell number and culture in drug-free media for 10 days. The area of plate coverage is depicted on the right, n = 3 biological replicates. ***p < 0.001. ( C ) Colony forming assay in SKOV3 cells transfected with empty vector (EV) or p53 vector encoding R175H or R273H, cultured with vehicle or 10 μM Fulvestrant for 7 days. The area of plate coverage is depicted on the right, n = 3 biological replicates. **p < 0.01. ( D ) EdU staining in PEO1 cells transfected with non-targeting control (siNC) or sip53 for 24 hours, followed by treatment with vehicle or 10 μM Fulvestrant treatment for 48 hours. The bar graph shows quantification of the average percentage of EdU positive cells per field. n = 9 fields from 3 biological repeats. Scale bar = 25 μm. ***p < 0.001. ( E ) PEO1 cells transfected with non-targeting control (siNC) or sip53 for 48 hours were treated with 10 μM Fulvestrant for 24 hours and grown as spheroids. Depicted data are representative of three independent experiments. Scale bar = 50 μm. Right panel: Violin plot of spheroid size following fulvestrant treatment. ***p<0.001. ( F ) Calcein staining for live cells in PEO1-pLKO.1 cells and PEO1-shp53 grown as organoids, following treatment with 3 μM Elacestrant. Right panel: Graph of calcein fluorescence relative to control (untreated) in PEO1-pLKO.1 and PEO1-shp53 cells following treatment with Elacestrant. The depicted data represent two independent biological replicates and fifteen technical replicates for each condition.
Techniques Used: Mutagenesis, Transfection, Control, Western Blot, Plasmid Preparation, Cell Culture, Staining, Fluorescence
Figure Legend Snippet: ( A ) Heatmap depicting differentially expressed genes in PEO1 cells stably-infected with pLKO.1 (Control) and shp53 cells treated with 10 μM Fulvestrant for 48 hours. n = 3 biological replicates. ( B ) Ingenuity pathway analysis of genes that are more responsive in shp53 cells compared to pLKO.1 cells in response to Fulvestrant. Shown are the top pathways significantly activated (red) and inhibited (blue) following Fulvestrant treatment in shp53 cells. Threshold Z score > 2. ( C ) Gene set enrichment analysis (GSEA) shows cell cycle related signature genes are differently expressed in shp53 cells compared to pLKO.1 cells in response to Fulvestrant. ( D ) Cell cycle analysis in pLKO.1 and shp53 stably infected PEO1 cells treated with 10 μM Fulvestrant for 48 hours. The right panel depicts quantification from four biological replicates. ***p<0.001. ( E ) Cell cycle analysis in pLKO.1 and shp53 stably infected PEO1 cells treated with 3 μM Elacestrant for 48 hours. The right panel depicts quantification from four biological replicates. ***p<0.001.
Techniques Used: Mutagenesis, Gene Expression, Stable Transfection, Infection, Control, Cell Cycle Assay
Figure Legend Snippet: ( A ) Western blot analysis for p53, p27Kip1 (p27) and GAPDH in PEO1 cells transfected with siNC or sip53 and then treated with 10 μM Fulvestrant or 3 μM Elacestrant for 48 hours. Data are representative of three independent experiments; densitometry values are normalized to siNC and loading control. ( B ) qPCR analysis of CDKN1B expression in PEO1 cells transfected with siNC or sip53 and then treated with 10 μM Fulvestrant or 3 μM Elacestrant for 48 hours. n = 3 biological replicates. N.S.: not significant. ( C ) qPCR analysis of SKP2 expression in PEO1 cells stably infected with vector alone (pLKO.1) or shp53 treated with vehicle or 10 μM Fulvestrant or 3 μM Elacestrant for 48 hours. n = 3 biological replicates. *p<0.05, **p<0.01, ***p<0.001. ( D ) Western blot for p53, SKP2 and GAPDH in PEO1 cells stably infected with vector alone (pLKO.1) or shp53 and treated with vehicle or 10 μM Fulvestrant or 3 μM Elacestrant for 48 hours. Data are representative of three independent experiments; quantification of the data depicted is shown for SKP2. Densitometry values are normalized to pLKO.1 and loading control. ( E ) Cell cycle analysis in shp53 PEO1 cells transfected with siNC or sip27 for 24 hours and then treated with 10 μM Fulvestrant for 48 hours. The right panel depicts quantification from four biological replicates. ** p<0.01, ***p<0.001. ( F ) Cell cycle analysis in shp53 PEO1 cells transfected with siNC or sip27 for 24 hours and then treated with 3 μM Elacestrant for 48 hours. The right panel depicts quantification from four biological replicates. *p<0.05, ***p<0.001. ( G ) Model for the impact of mutant p53 on endocrine sensitivity.
Techniques Used: Expressing, Mutagenesis, Western Blot, Transfection, Control, Stable Transfection, Infection, Plasmid Preparation, Cell Cycle Assay