CAS: 859212-16-1; (S)-N-(3-([4,5'-Bipyrimidin]-2-Ylamino)-4-Methylphenyl)-4-((3-(Dimethylamino)Pyrrolidin-1-yl)Methyl)-3-(Trifluoromethyl)Benzamide

该化合物是一种小分子抑制剂,主要用于治疗某些类型的癌症,特别是慢性流线性白血病(CML)和急性淋巴性白血病(ALL),它有选择性地抑制BCR-ABL抗结核性血管酶,这是一种聚变蛋白质,在这些白血病的发病中起着关键作用.Bafetinib的化学配方反映了其复杂结构,包括多种功能组,有助于其药理活动.它的特点是它能够抑制细胞扩散,在表现BCR-ABL聚变蛋白的癌症细胞中诱发骨缩.Bfetinib是口头施用,以其相对有利的药理皮肤特征而著称,包括良好的生物利用率.然而,与许多有针对性的治疗方法一样,它可能与副作用有关,其中可能包括外观毒性和其他器官特有影响.持续的研究继续探索其在各种临床环境中的功效和安全性,以及其在混合疗法中的潜在用途.

结构式图片

上下游产品

4-(Bromomethyl)-3-Trifluoromethyl-N-{4-Methyl-3-[4-(5-Pyrimidinyl)Pyrimidin-2-Ylamino]Phenyl}Benzamide 859213-40-4

合成工艺路线路线简述

  • 641615-36-3 + 261952-01-6 = 859212-16-1
    反应条件:1.1 Reagents: Sodium Bisulfite,Sodium Bromate Solvents: Ethyl Acetate1.2 Reagents: Oxalyl Chloride Catalysts: Dimethylformamide Solvents: Dichloromethane; Rt1.3 Reagents: Potassium Carbonate Solvents: 1,4-Dioxane; Reflux2.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; Rt
    标题:Design And Synthesis Of 3-Substituted Benzamide Derivatives As Bcr-Abl Kinase Inhibitors
    作者:Asaki,Tetsuo; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2006 卷标:16(5) 页码:1421-1425]

    132883-44-4 + 859213-40-4 = 859212-16-1
    反应条件:1.1 Reagents: Potassium Carbonate Solvents: Dimethylformamide; Rt
    标题:Design And Synthesis Of 3-Substituted Benzamide Derivatives As Bcr-Abl Kinase Inhibitors
    作者:Asaki,Tetsuo; Et Al
    参考文献:Bioorganic & Medicinal Chemistry Letters 日期:2006 卷标:16(5) 页码:1421-1425
📜4-甲基-3-(三氟甲基)苯甲酸置于sodium Bromate,草酰氯,Potassium Carbonate,Sodium Hydrogensulfite,N,N-二甲基甲酰胺体系中,用 1,4-二氧六环,二氯甲烷,乙酸乙酯,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 巴氟替尼
参考文献:Design And Synthesis Of 3-Substituted Benzamide Derivatives As Bcr-Abl Kinase Inhibitors
标题:Design And Synthesis Of 3-Substituted Benzamide Derivatives As Bcr-Abl Kinase Inhibitors
摘要:A Series Of 3-Substituted Benzamide Derivatives Structurally Related To Sti-571 (Imatinib Mesylate),A Bcr-Abl Tyrosine Kinase Inhibitor Used To Treat Chronic Myeloid Leukemia (Cml),Was Prepared And Evaluated For Antiproliferative Activity Against The Bcr-Abl-Positive Leukemia Cell Line K562. About Ten 3-Halogenated And 3-Trifluoromethylated Benzamide Derivatives Were Identified As Highly Potent Bcr-Abl Kinase Inhibitors. One Of These,Ns-187 (9B),Is A Promising New Candidate Bcr-Abl Inhibitor For The Therapy Of Sti-571-Resistant Chronic Myeloid Leukemia. (C) 2005 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2005.11.042

海关参考信息

专利信息


专利号:US-12240835-B2
优先权日:2018-09-18
标题:Substituted benzamides as intermediates in the synthesis of inhibitors of tyrosine kinase enzymatic activity
发明人:ROMERO F ANTHONY; KIRSCHBERG THORSTEN A; HALCOMB RANDALL; XU YINGZI
权利人:TERNS PHARMACEUTICALS INC
摘要:Provided herein are compounds, preferably compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, compositions thereof, and methods of their preparation, and methods of inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, and methods for treating diseases wherein modulation of BCR-ABL1 activity prevents, inhibits, or ameliorates the pathology and/or symptomology of the disease. Intermediates such as compounds of Formula (S23), which are useful in the synthesis of compounds inhibiting tyrosine kinase enzymatic activity of a protein selected from Abelson protein (ABL1), Abelson-related protein (ABL2), or a chimeric protein BCR-ABL1, are also provided.

专利号:US-11759496-B2
优先权日:2016-05-10
标题:Compounds and pharmaceutical use thereof in the treatment of cancer
发明人:SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE
权利人:KAROYAN PHILIPPE
摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.

专利号:WO-2024117980-A1
优先权日:2022-12-02
标题 :Compounds for modulating src family kinases and uses thereof
发明人:KUMAR ALAN PREM; SETHI GAUTAM; LEE E HUI CLARISSA; - BASAPPA; RANGAPPA KANCHUGARAKOPPAL S; MOHAN CHAKRABHAVI DHANANJAYA
权利人:NAT UNIV SINGAPORE; UNIV OF MYSORE
摘要:The present invention relates to chalcone (CHL) compounds, their synthesis, and applications in modulating the activity of Src Family Kinases (SFKs), specifically Lyn kinase, and methods of use in treating various diseases and conditions associated with aberrant activity of Src Family Kinases.

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主要参考文献


1: Chen X, Du Q, Guo H, He Q, Yang B, Ding L. Bafetinib Suppresses the Transcription of PD-L1 Through c-Myc in Lung Cancer. Front Pharmacol. 2022 Jun 2;13:897747. doi: 10.3389/fphar.2022.897747.
2: Santos FP, Kantarjian H, Cortes J, Quintas-Cardama A. Bafetinib, a dual Bcr- Abl/Lyn tyrosine kinase inhibitor for the potential treatment of leukemia. Curr Opin Investig Drugs. 2010 Dec;11(12):1450-65. 715(1-3):172-80. doi: 10.1016/j.ejphar.2013.05.025. Epub 2013 Jun 6.
6:25694. doi: 10.1038/srep25694.

合成参考文献


参考文献:10.1007/s00216-011-5207-9
摘要:Kool J, Jonker N, Irth H, Niessen WMA. Studying protein–protein affinity and immobilized ligand–protein affinity interactions using MS-based methods. Analytical and Bioanalytical Chemistry. 2011 Jul 14;401(4):1109. doi: 10.1007/s00216-011-5207-9.
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