H3B-6545 hydrochloride
Modify Date: 2025-08-25 18:24:03
H3B-6545 hydrochloride structure
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Common Name | H3B-6545 hydrochloride | ||
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| CAS Number | 2052132-51-9 | Molecular Weight | 604.04 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C30H30ClF4N5O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of H3B-6545 hydrochlorideH3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA). |
| Name | H3B-6545 Hydrochloride |
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| Description | H3B-6545 Hydrochloride is an oral, selective estrogen receptor covalent antagonist (SERCA). |
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| 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 |
| Molecular Formula | C30H30ClF4N5O2 |
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| Molecular Weight | 604.04 |