H3B-6545 - 10mM in DMSO , CAS No.2052130-80-8

CAS: 2052130-80-8 Cat. No.: H654751 분자식: C₃₀H₂₉F₄N₅O₂ 분자량: 567.58 PubChem CID: 124091040

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

H3B-6545 is an oral, selective estrogen receptor covalent antagonist ( SERCA ) for the research of metastatic ER-positive, HER2-negative breast cancer

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 GI 50 s 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:Estrogen receptor

Specifications

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

H3B-6545 is an oral, selective estrogen receptor covalent antagonist ( SERCA ) for the research of metastatic ER-positive, HER2-negative breast cancer.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

ANTAGONIST

이름과 식별자

PubChem CID

124091040

MeSH 용어

((2E)-N,N-dimethyl-4-((2-((5-((1Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenylbut-1-en-1-yl)pyridin-2-yl)oxy)ethyl)amino)but-2-enamide) hydrochloride salt;H3B-6545

분자량

567.58

자주 묻는 질문

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 2052130-80-8, the molecular formula is C30H29F4N5O2, and the molecular weight is 567.58 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.