CAS: 2114339-57-8; (S)-8-(2,4-Dichlorophenyl)-9-(4-((1-(3-Fluoropropyl)Pyrrolidin-3-yl)Oxy)Phenyl)-6,7-Dihydro-5H-Benzo[7]Annulene-3-Carboxylic Acid
该化合物是用于治疗雌激素受体阳性(ER+)乳腺癌的调查性选择性雌激素受体降解器(SERD),对雌激素受体有约束力并降低其人格,从而抑制依赖雌激素的肿瘤生长.Amercenestrant展示了高口腔生物利用率和强力对抗性活动,甚至在ESR1-雌性癌症中也是如此,这些癌症往往对标准的内分泌疗法具有抗药性.它的药理和基因特征支持了一次日服药,加强了病人的合规性.临床和临床研究表明,在早期和高级ER+乳腺癌环境中都有可能应用这种药物.正在进行的研究旨在进一步阐明其治疗潜力和在更广泛的病人群体中的安全性.
- 英文名称(S)-8-(2,4-Dichlorophenyl)-9-(4-((1-(3-Fluoropropyl)Pyrrolidin-3-yl)Oxy)Phenyl)-6,7-Dihydro-5H-Benzo[7]Annulene-3-Carboxylic Acid
- 中文名称(S)-8-(2,4-二氯苯基)-9-(4-((1-(3-氟丙基)吡咯烷-3-基)氧基)苯基)-6,7-二氢-5H-苯甲酸[7]苯并-3-吡唑羧酸
- IUPAC名称(S)-8-(2,4-dichlorophenyl)-9-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)oxy)phenyl)-6,7-dihydro-5H-benzo[7]annulene-3-carboxylic acid
- CAS编号2114339-57-8
- MFCD编号:MFCD32693904
- FDA UNII编号:TBF1NHY02O
- 分子式:C31H30Cl2FNO3分子量:554.49
- 产品CID: 1093372
- 产品分类Inhibitors/Agonists → Endocrinology/Hormones → ERR | Aliphatic Heterocycles
物理性质
- 沸点676.7±55.0 °C(预测)
- 密度1.297±0.06 g/cm3(预测)
- pKa:4.18±0.20(预测)
- LogP:5.3
- 溶解性DMSO:100.0(Max Conc. mg/mL);180.35(Max Conc. Mm)
- 外观形态白色至类白色固体
- 储存条件Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
- 产品应用该化合物是口服的,非小类选择性雌性激素受体降解器(SERD),具有潜在的抗抗抗菌素活动;它作为强雌性体受体(ER)对立体,在ERΑ降解时表现出0.2 NM的EC50.
合成工艺路线路线简述
海关参考信息
- 2901210000-乙烯
2901220000-丙烯
2902500000-苯乙烯
2902600000-乙苯 - 💡 提示：海关信息按照顺序优先匹配，如需确认的海关信息，请参考相关资料。
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供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
1: Tamura K, Mukohara T, Yonemori K, Kawabata Y, Nicolas X, Tanaka T, Iwata H. Phase 1 study of oral selective estrogen receptor degrader (SERD) amcenestrant (SAR439859), in Japanese women with ER-positive and HER2-negative advanced breast cancer (AMEERA-2). Breast Cancer. 2023 May;30(3):506-517. doi: 10.1007/s12282-023-01443-8. Epub 2023 Mar 29.
2: Bardia A, Chandarlapaty S, Linden HM, Ulaner GA, Gosselin A, Cartot-Cotton S, Cohen P, Doroumian S, Paux G, Celanovic M, Pelekanou V, Ming JE, Ternès N, Bouaboula M, Lee JS, Bauchet AL, Campone M. AMEERA-1 phase 1/2 study of amcenestrant, SAR439859, in postmenopausal women with ER-positive/HER2-negative advanced breast cancer. Nat Commun. 2022 Jul 15;13(1):4116. doi: 10.1038/s41467-022-31668-8.
3: Bardia A, Cortes J, Hurvitz SA, Delaloge S, Iwata H, Shao ZM, Kanagavel D, Cohen P, Liu Q, Cartot-Cotton S, Pelekanou V, O'Shaughnessy J. AMEERA-5: a randomized, double-blind phase 3 study of amcenestrant plus palbociclib versus letrozole plus palbociclib for previously untreated ER+/HER2- advanced breast cancer. Ther Adv Med Oncol. 2022 Mar 15;14:17588359221083956. doi: 10.1177/17588359221083956.
合成参考文献
参考文献:10.3390/ijms22157812
摘要:Hernando C, Ortega-Morillo B, Tapia M, Moragón S, Martínez MT, Eroles P, Garrido-Cano I, Adam-Artigues A, Lluch A, Bermejo B, Cejalvo JM. Oral Selective Estrogen Receptor Degraders (SERDs) as a Novel Breast Cancer Therapy: Present and Future from a Clinical Perspective. Int J Mol Sci. 2021 Jul 22;22(15).
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