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H3B-6545

Catalog No. T11530L CAS 2052130-80-8

H3B-6545 is an oral and selective antagonist of estrogen receptor covalent (SERCA).

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H3B-6545, CAS 2052130-80-8

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,140.00
50 mg	8-10 weeks	$ 1,490.00
100 mg	8-10 weeks	$ 2,530.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	H3B-6545 is an oral and selective antagonist of estrogen receptor covalent (SERCA).
In vitro	H3B-6545 inhibits ERαWT activity and growth of ERαWT -positive breast cancer lines and it also effectively inhibits ERαWT activity and suppresses proliferation of ERαWT -positive breast cancer lines (GI50s: 0.3-0.4, 1.0, 0.5, 5.2, and 0.2 nM for MCF7, HCC1428, BT483, T47D, and CAMA-1 cell lines). H3B-6545 is a first-in-class selective ER covalent antagonist (SERCA). H3B-6545 is a highly selective small molecule. In biochemical and cell-based assays, it also effectively antagonizes wild-type and mutant ERα. In vitro comparisons with the 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 refers to as selective ER covalent antagonist (SERCA), which inactivates both wild-type and mutant ERα by targeting C530 and enforcing a unique antagonist conformation [1].
In vivo	H3B-6545 is well tolerated across a broad dose range and at exposures that significantly exceed those required for efficacy in mouse xenograft models. H3B-6545 (once daily; p.o.) treatment, displays effective 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. H3B-6545 displays superior antitumor activity to Tamoxifen and Fulvestrant in patient-derived xenograft models of estrogen receptor-positive breast cancer including models carrying ERα mutations in rats and monkeys [1].

Molecular Weight	567.58
Formula	C30H29F4N5O2
CAS No.	2052130-80-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

H3B-6545 2052130-80-8 Others H3B6545 H3B 6545 H-3B-6545 inhibitor inhibit

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