2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)-
![2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Structure](CAS/20210305/GIF/2369048-69-9.gif)
- CAS No.
- 2369048-69-9
- Chemical Name:
- 2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)-
- Synonyms
- GNE-274;2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)-
- CBNumber:
- CB89825620
- Molecular Formula:
- C29H31NO4
- Molecular Weight:
- 457.56
- MDL Number:
- MOL File:
- 2369048-69-9.mol
2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Chemical Properties,Uses,Production
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
Raw materials
Preparation Products
2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Aladdin Scientific | +1-+1(833)-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3453 | 58 |
| Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd | 15317229551 | 15151849396@163.com | China | 997 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 28118 | 58 |