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1953132-75-6

1953132-75-6 structure

1953132-75-6 structure

Name: GNE-149
Chemical Name: GNE-149
CAS Number: 1953132-75-6
Molecular Formula: C₂₈H₃₃F₄N₃O
Molecular Weight: 503.57
Catalog: Research Areas Cancer
Create Date: 2022-03-26 23:06:06
Modify Date: 2026-07-01 18:52:41
GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].

Name	GNE-149
Synonyms	1H-Pyrido[3,4-b]indole, 1-[2,6-difluoro-4-[[1-(3-fluoropropyl)-3-azetidinyl]oxy]phenyl]-2-(2-fluoro-2-methylpropyl)-2,3,4,9-tetrahydro-3-methyl-, (1R,3R)

Description	GNE-149 is an orally bioavailable full antagonist of estrogen receptor α (ERα; IC50=0.053 nM). GNE-149 is a selective estrogen receptor degrader (SERD). GNE-149 can be used for the research of breast cancer[1].
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	ERα:0.053 nM (IC50)
In Vitro	GNE-149 exhibits antiproliferative activity in MCF7 and T47D cells with IC50s of 0.66 and 0.69 nM, respectively[1]. GNE-149 exhibits ERα Degradation in MCF7 and T47D cells with IC50s of 0.053 and 0.031 nM, respectively[1].
In Vivo	GNE-149 (0.3-30 mg/kg) exhibits in vivo efficacy in an MCF7 xenograft mouse model harboring either wild-type (WT) ERα or overexpressed Y537S mutant[1]. GNE-149 has favorable pharmacokinetic profile, including total clearance (CL; 19, 8, and 13 mL/min/kg for Rat, Dog, and Cyno) and oral bioavailability (F; 31%, 49%, and 28% for Rat, Dog, and Cyno)[1]. Animal Model: Female Crl:NU Foxn1 nu mice (at 7 weeks of age) bearing wild-type (WT) ERαor overexpressed Y537S mutant MCF7 tumor[1] Dosage: 0.3, 1, 3, 10, and 30 mg/kg Administration: Orally q.d. for 21 days Result: Exhibited dose-dependent efficacy in the MCF7 WT and Y537S mutant xenograft model, with tumor regression observed at all doses above 0.3 mg/kg in Y537S mutant xenograft model.
References	[1]. Jun Liang, et al. Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer. ACS Med Chem Lett. 2020 May 26;11(6):1342-1347.

Molecular Formula	C₂₈H₃₃F₄N₃O
Molecular Weight	503.57

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