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H3B-6545 hydrochloride

CAS No. : 2052132-51-9

MCE 站：H3B-6545 hydrochloride

产品活性：H3B-6545 hydrochloride 是一种有效的，具有口服活性的选择性雌激素受体共价拮抗剂 (SERCA)。H3B-6545 hydrochloride 可用于研究转移性 ER 阳性，HER2 阴性乳腺癌。

研究领域：Vitamin D Related/Nuclear Receptor

作用靶点：Estrogen Receptor/ERR

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. 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 ERα^WT activity ａnd growth of ERα^WT -positive breast cancer lines. H3B-6545 potently inhibits ERα^WT activity ａnd suppresses proliferation of ERα^WT -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.

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.

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