GNE-274
Modify Date: 2025-08-27 10:07:16
GNE-274 structure
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Common Name | GNE-274 | ||
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| CAS Number | 2369048-69-9 | Molecular Weight | 457.56 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C29H31NO4 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of GNE-274GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research[1][2]. |
| Name | GNE-274 |
|---|
| Description | GNE-274 is a non-degrader that is structurally related to GDC-0927 (ER degrader). GNE-274 does not induce ER turnover and functions as a partial ER agonist in breast cancer cell lines. GNE-274 increase chromatin accessibility at ER-DNA binding sites, while GDC-0927 do not. GNE-274 is a potent inhibitor of ER-ligand binding domain (LBD). GNE-274 can be used for cancer research[1][2]. |
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| Related Catalog | |
| In Vitro | GNE-274 (0.1 nM-1000 nM; 4 hours) fails to trigger increased ER turnover in MCF7, MD-134, HCC1500 and CAMA cells[1]. GNE-274 (1-1000 nM; 7-10 days) potently inhibits cellular proliferation, exhibiting greater potency than fulvestrant, 4-OHT, AZD9496, and GDC-0810 in E2-stimulated ER+ breast cancer cell lines[1]. In transposaseaccessible chromatin sequencing (ATAC-seq) assay, GNE-274 increase chromatin accessibility at ER-DNA binding sites, it significantly alters chromatin accessibility at 594 sites. But GDC-0927 has considerably less impact on chromatin accessibility[1]. Cell Viability Assay[1] Cell Line: MCF7, MB-134, HCC1500, EFM-19, CAMA-1, T-47D cells Concentration: 1 nM; 10 nM; 100 nM; 1000 nM Incubation Time: 7-10 days Result: Exhibited IC50 values approximately ranging from 5nM to 20 nM in different cells. |
| References |
| Molecular Formula | C29H31NO4 |
|---|---|
| Molecular Weight | 457.56 |