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ChemicalBook >> CAS DataBase List >>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)-

2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Structure
2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- structure
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
MSDS File:
SDS
Last updated:2025-04-17 18:22:24
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2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- 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)- price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ChemScene CS-0181241 GNE-274 98.00% 2369048-69-9 1mg $325 2026-06-04 Buy
ChemScene CS-0181241 GNE-274 98.00% 2369048-69-9 5mg $975 2026-06-04 Buy
ChemScene CS-0181241 GNE-274 98.00% 2369048-69-9 10mg $1571 2026-06-04 Buy
ChemScene CS-0181241 GNE-274 98.00% 2369048-69-9 25mg $3250 2026-06-04 Buy
ChemScene CS-0181241 GNE-274 98.00% 2369048-69-9 50mg $5200 2026-06-04 Buy
Product number Packaging Price Buy
CS-0181241 1mg $325 Buy
CS-0181241 5mg $975 Buy
CS-0181241 10mg $1571 Buy
CS-0181241 25mg $3250 Buy
CS-0181241 50mg $5200 Buy

2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- Chemical Properties, Uses, Production

Uses

GNE-274 is a structural analog of the ER degrader GDC-0927 and is a non-degrader. GNE-274 does not induce conversion of ER in breast cancer cell lines and functions as a partial ER agonist (partial ER agonist). GNE-274 increases the chromatin accessibility of ER-DNA binding sites, whereas GDC-0927 does not. GNE-274 is an effective ER ligand binding domain (LBD) inhibitor. GNE-274 can be used in cancer research.

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

Global Suppliers ( 5)
Supplier Tel Email Country ProdList Advantage
BOC Sciences 1-631-485-4226; 16314854226 info@bocsci.com United States 9920 65
ShangHai Caerulum Pharma Discovery Co., Ltd. 18149758185 18149758185 sales-cpd@caerulumpharma.com China 3493 58
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd 15317229551 15151849396@163.com China 959 58
TargetMol Chemicals Inc. 4008200310 15002144251 marketing@tsbiochem.com China 24951 58
Aladdin Scientific tp@aladdinsci.com United States 50068 58
Supplier Advantage
BOC Sciences 65
ShangHai Caerulum Pharma Discovery Co., Ltd. 58
Suzhou youruike Chemical Pharmaceutical Technology Co., Ltd 58
TargetMol Chemicals Inc. 58
Aladdin Scientific 58

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2H-1-Benzopyran-6-ol, 3-(3-hydroxyphenyl)-4-methyl-2-[4-[(1-propyl-3-azetidinyl)methoxy]phenyl]-, (2S)- GNE-274 2369048-69-9