| Identification | Back Directory | [Name]
2-Butenamide, N,N-dimethyl-4-[[2-[[5-[(1Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]-2-pyridinyl]oxy]ethyl]amino]-, (2E)- | [CAS]
2052130-80-8 | [Synonyms]
H3B-6545
H3B6545,H-3B-6545,H3B 6545
2-Butenamide, N,N-dimethyl-4-[[2-[[5-[(1Z)-4,4,4-trifluoro-1-(3-fluoro-1H-indazol-5-yl)-2-phenyl-1-buten-1-yl]-2-pyridinyl]oxy]ethyl]amino]-, (2E)- | [Molecular Formula]
C30H29F4N5O2 | [MDL Number]
MFCD31692408 | [MOL File]
2052130-80-8.mol | [Molecular Weight]
567.58 |
| Chemical Properties | Back Directory | [Boiling point ]
702.0±60.0 °C(Predicted) | [density ]
1.286±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.02±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
H3B-6545 is an oral, selective estrogen receptor covalent antagonist (SERCA) for the research of metastatic ER-positive, HER2-negative breast cancer[1][2]. | [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]
[1] Peter G. Smith, et al. Abstract DDT01-04: Discovery and development of H3B-6545: A novel, oral, selective estrogen receptor covalent antagonist (SERCA) for the treatment of breast cancer.AACR Annual Meeting 2017; April 1-5.
[2] Amy H Kim, et al. H3B-6545, a selective estrogen receptor covalent antagonist, prevents bone loss in ovariectomized Sprague-Dawley rats. J Pharmacol Toxicol Methods. Sep-Oct 2019;99:106595. |
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| Company Name: |
Wuhan Topule
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+86-02787215551 19945035818 |
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http://www.topule.com/ |
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