Shanghai Nianxing Industrial Co., Ltd
China
Product Name: H3B-6545 hydrochloride
Price:
Purity: 98.0%
Stocking Period: 10 Day
Contact: Yang

DC Chemicals Limited
China
Product Name: H3B-6545 hydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

2052132-51-9

2052132-51-9 structure

2052132-51-9 structure

Name: H3B-6545 hydrochloride
Chemical Name: H3B-6545 Hydrochloride
CAS Number: 2052132-51-9
Molecular Formula: C₃₀H₃₀ClF₄N₅O₂
Molecular Weight: 604.04
Catalog: Research Areas Cancer
Create Date: 2019-02-08 11:45:44
Modify Date: 2024-01-03 23:19:35
H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).

Name	H3B-6545 Hydrochloride

Description	H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).
Related Catalog	Signaling Pathways >> Others >> Estrogen Receptor/ERR Research Areas >> Cancer
Target	Estrogen receptor[1]
In Vitro	H3B-6545 is a highly selective small molecule that potently antagonizes wild-type and mutant ERα in biochemical and cell based assays. In vitro comparisons with standard of care and other experimental agents confirm increased cell potency of H3B-6545 under continuous as well as washout treatment conditions[1]. H3B-6545, a member of a novel class of ERα antagonists refer to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation. H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). H3B-6545 inhibits ERαWT activity and growth of ERαWT -positive breast cancer lines. H3B-6545 potently inhibits ERαWT activity and suppresses proliferation of ERαWT -positive breast cancer lines. With GI50s of 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D and CAMA-1 cell lines[1].
In Vivo	In vivo, once daily oral dosing of H3B-6545 shows potent activity and superior efficacy to fulvestrant in the MCF-7 xenograft model with maximal antitumor activity at doses >10x below the maximum tolerated dose in mice. In addition, H3B-6545 shows superior antitumor activity to Tamoxifen and Fulvestrant in patient derived xenograft models of estrogen receptor positive breast cancer including models carrying ERα mutations in rat and monkeys, H3B-6545 is well tolerated across a broad dose range and at exposures that significantly exceed those required for efficacy in mouse xenograft models[1].
References	[1]. Peter G. Smith, et al. Abstract DDT01-04: Discovery and development of H3B-6545: A novel, oral, selective estrogen receptor covalent antagonist (SERCA) for the treatment of breast cancer.AACR Annual Meeting 2017; April 1-5. [2]. Manav Korpal, et al. Development of a First-in-Class Oral Selective ER Covalent Antagonist (SERCA) for the Treatment of ERα^WT and ERα^MUT Breast Cancer.

Molecular Formula	C₃₀H₃₀ClF₄N₅O₂
Molecular Weight	604.04