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  3. H3B-6545 Hydrochloride

H3B-6545 Hydrochloride 

Cat. No.: HY-112596A
Handling Instructions

H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA).

For research use only. We do not sell to patients.

H3B-6545 Hydrochloride Chemical Structure

H3B-6545 Hydrochloride Chemical Structure

CAS No. : 2052132-51-9

Size Price Stock
10 mM * 1  mL in DMSO USD 465 Ask For Quote & Lead Time
5 mg USD 350 Ask For Quote & Lead Time
10 mg USD 600 Ask For Quote & Lead Time
50 mg USD 1800 Ask For Quote & Lead Time
100 mg USD 3050 Ask For Quote & Lead Time

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H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA)[1].

IC50 & 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].

Clinical Trial
Molecular Weight









Room temperature in continental US; may vary elsewhere.


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H3B-6545Estrogen Receptor/ERRInhibitorinhibitorinhibit

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