| Company Name: |
TargetMol Chemicals Inc.
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| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:GNE-274
CAS:2369048-69-9
Purity:详情请点击官网 Package:1 mg
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| | 2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Basic information |
| | 2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Chemical Properties |
| Boiling point | 644.2±55.0 °C(Predicted) | | density | 1.210±0.06 g/cm3(Predicted) | | pka | 9.83±0.10(Predicted) | | form | Solid | | color | Off-white to light yellow |
| | 2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Usage And Synthesis |
| Biological Activity | 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].
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]. | | References | [1]. Jane Guan, et al. Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility. Cell. 2019 Aug 8;178(4):949-963.e18.[2]. Jane Guan, et al. Abstract NG05: Not all "SERDs" are equal: Context-independent ER degradation and full ER antagonism define the next generation of ER therapeutics. Cancer research. |
| | 2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Preparation Products And Raw materials |
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