CAS: 1035270-39-3; Rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-Pyrazol-3-yl)-4-((3R,5S)-3,5-Dimethylpiperazin-1-yl)Benzamide
该化合物是一种小分子抑制剂,主要针对纤维生长系数受体(FGFR)家族,特别是FGFR1,FGFR2和FGFR3.它被归类为选择性的抗抑郁剂,并已调查其在各种癌症中的潜在治疗用途,特别是FGFR畸变.该化合物展示了一种具体的行动机制,阻断了FGFR的磷酸,从而抑制了促进肿瘤生长和生存的下游信号路径.AZD-4547通常通过口头管理,并在临床试验中评估其在治疗诸如膀胱癌和其他固态肿瘤等条件下的效果和安全性特征.其化学结构包括一个核心,允许对FGFRs的高亲近性和选择性,使其成为目标癌症疗法的一个对象.与许多调查药物一样,正在进行的研究继续探索其全部潜力,包括抗药机制和组合疗法,以提高其效力.
- 英文名称Rel-N-(5-(3,5-Dimethoxyphenethyl)-1H-Pyrazol-3-yl)-4-((3R,5S)-3,5-Dimethylpiperazin-1-yl)Benzamide
- 中文名称rel-N-[5-[2-(3,5-二甲氧基苯基)乙基]-1H-吡唑-3-基]-4-[(3R,5S)-3,5-二甲基-1-哌嗪基]苯甲酰胺
- IUPAC名称N-(5-(3,5-dimethoxyphenethyl)-1H-pyrazol-3-yl)-4-((3R,5S)-3,5-dimethylpiperazin-1-yl)benzamide
- 其它别名rel-N-[5-[2-(3,5-Dimethoxyphenyl)ethyl]-1H-pyrazol-3-yl]-4-[(3R,5S)-3,5-dimethyl-1-piperazinyl]benzamide
- CAS编号1035270-39-3
- MFCD编号:MFCD22580423
- EINECS号:681-057-4
- FDA UNII编号:2167OG1EKJ
- 分子式:C26H33N5O3
- 分子量:463.58
- 产品CID: 69990
- 同类组份化合物CAS1035270-39-31394854-62-6
- 产品分类Protein Tyrosine Kinase/RTK → FGFR | Protein Tyrosine Kinase/RTK → VEGFR
物理性质
MSDS等安全信息
欧盟法规
ECHA物质C&L通报上下游产品
3,5-dimethoxybenzaldehdye (E)-3,5-dimethoxycinnamic acid 4-fluorobenzoic acid ethyl ester cis-2,6-dimethylpiperazine合成工艺路线路线简述
专利信息
专利号:US-2022411407-A1
优先权日:2019-11-15
标题:Aryl aminopyrimidines as dual mertk and tyro3 inhibitors and methods thereof
发明人：WANG XIAODONG; ZHOU YUBAI; DING RANSHENG; KONG DEYU; FRYE STEPHEN
权利人:UNIV NORTH CAROLINA CHAPEL HILL
摘要:Aminopyrimidine containing compounds that inhibit both Mer tyrosine kinase (MerTK) activity and Tyro3 kinase activity are disclosed herein. Additionally disclosed are methods of synthesis and use of the aminopyrimidine containing compounds as anti-cancer agents, immunostimulatory and immunomodulatory agents, anti-platelet agents, anti-infective agents, and as adjunctive agents.
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主要参考文献
1: Ramsey MR, Wilson C, Ory B, Rothenberg SM, Faquin W, Mills AA, Ellisen LW. FGFR2 signaling underlies p63 oncogenic function in squamous cell carcinoma. J Clin Invest. 2013 Aug 1;123(8):3525-38. doi: 10.1172/JCI68899. Epub 2013 Jul 8.
2: Fox EM, Kuba MG, Miller TW, Davies BR, Arteaga CL. Autocrine IGF-I/insulin receptor axis compensates for inhibition of AKT in ER-positive breast cancer cells with resistance to estrogen deprivation. Breast Cancer Res. 2013 Jul 11;15(4):R55. [Epub ahead of print] doi: 10.1038/oncsis.2013.4.
5: Xie L, Su X, Zhang L, Yin X, Tang L, Zhang X, Xu Y, Gao Z, Liu K, Zhou M, Gao B, Shen D, Zhang L, Ji J, Gavine PR, Zhang J, Kilgour E, Zhang X, Ji Q. FGFR2 gene amplification in gastric cancer predicts sensitivity to the selective FGFR inhibitor AZD4547. Clin Cancer Res. 2013 May 1;19(9):2572-83. doi: 10.1158/1078-0432.CCR-12-3898. Epub 2013 Mar 14. doi: 10.1139/cjpp-2012-0234. Epub 2013 Jan 21. doi: 10.1158/1078-0432.CCR-12-2694. Epub 2012 Oct 18. Erratum in: Clin Cancer Res. 2013 Jul 1;19(13):3714. Schöttle, Jakob [added]. doi: 10.1038/onc.2012.319. Epub 2012 Aug 6. doi: 10.1126/science.1220834. Epub 2012 Jul 26.
合成参考文献
参考文献:10.1124/mol.119.115964
摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964.
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