2052130-80-8
2052130-80-8 structure
- Name: H3B-6545
- Chemical Name: H3B-6545
- CAS Number: 2052130-80-8
- Molecular Formula: C30H29F4N5O2
- Molecular Weight: 567.58
- Catalog: Research Areas Cancer
- Create Date: 2019-02-09 11:58:02
- Modify Date: 2024-01-11 10:58:30
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H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA).
| Name | H3B-6545 |
|---|
| Description | H3B-6545 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 | C30H29F4N5O2 |
|---|---|
| Molecular Weight | 567.58 |