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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)- manufacturers
- H3B-6545
-
- $1130.00
-
2026-07-27
- CAS:2052130-80-8
- Purity:
- Supply Ability: 10g
- H3B-6545
-
- $1130.00
-
2026-07-27
- CAS:2052130-80-8
- Purity:
- Supply Ability: 10g
- H3B-6545
-
- $1130.00
-
2025-09-17
- CAS:2052130-80-8
- Purity:
- Supply Ability: 10g
|
| | 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)- Basic information |
| Product 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)- | | Synonyms: | 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)-;H3B-6545;H3B6545,H-3B-6545,H3B 6545;(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 | | CAS: | 2052130-80-8 | | MF: | C30H29F4N5O2 | | MW: | 567.58 | | EINECS: | | | Product Categories: | | | Mol File: | 2052130-80-8.mol | ![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)- Structure](CAS/20200401/GIF/2052130-80-8.gif) |
| | 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)- Chemical Properties |
| Boiling point | 702.0±60.0 °C(Predicted) | | density | 1.286±0.06 g/cm3(Predicted) | | pka | 12.02±0.40(Predicted) | | form | Solid | | color | Light yellow to yellow |
| | 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)- Usage And Synthesis |
| 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. |
| | 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)- Preparation Products And Raw materials |
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