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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
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 ERαWT and ERαMUT Breast Cancer.
Molecular Formula C30H30ClF4N5O2
Molecular Weight 604.04

Chemsrc provides CAS#:2052132-51-9 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 2052132-51-9 | Chemsrc address: https://www.chemsrc.com/en/baike/1556104.html

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