CAS: 790299-79-5; N-(4-Methyl-3-((4-(Pyridin-3-yl)Thiazol-2-yl)Amino)Phenyl)-4-((4-Methylpiperazin-1-yl)Methyl)Benzamide

该化合物是一种小分子的气旋性暴动酶抑制剂,主要以其在针对特定受体体强力强力体系,包括参与某些癌症和发炎性疾病的信号路径的人方面所发挥的作用而著称,其特点是它能够有选择地抑制诸如C-KIT等运动细胞的活动,这种运动与各种恶性疾病有关,并显示出在治疗狗中胸细胞肿瘤和某些人类癌症形式的病症方面的前景.Masitinib通常通过口服,具有有利的药用植物特征,允许有效的系统吸收.其行动机制包括阻断强力残留物的磷酸化,从而破坏下游信号路径,从而促进细胞扩散和生存.该综合体经历了各种临床试验,以评估其功效和安全性,显示了其在肿瘤学和免疫学方面的潜在好处.与许多有针对性的疗法一样,其副作用可能各不相同,但往往包括胃肠紊乱和血科变化.

英文名称N-(4-Methyl-3-((4-(Pyridin-3-yl)Thiazol-2-yl)Amino)Phenyl)-4-((4-Methylpiperazin-1-yl)Methyl)Benzamide
中文名称马赛替尼
IUPAC名称N-(4-methyl-3-((4-(pyridin-3-yl)thiazol-2-yl)amino)phenyl)-4-((4-methylpiperazin-1-yl)methyl)benzamide
其它别名4-((4-Methylpiperazin-1-yl)Methyl)-N-(4-Methyl-3-((4-Pyridin-3-Yl-1,3-Thiazol-2-yl)Amino)Phenyl)Benzamide; Masitinib [inn]; Masatinib; Masitinib; Mastinib; Masitinib [wh
CAS编号790299-79-5
MFCD编号:MFCD09954132
FDA UNII编号:M59NC4E26P
分子式:C28H30N6OS
分子量:498.66
产品CID: 1784130
同类组份化合物CAS1048007-93-7 (mesylate)790299-79-5 (free base)
产品分类生物化工 → 抑制剂 → 蛋白酪氨酸激酶

相似结构搜索
InChIKey: WJEOLQLKVOPQFV-UHFFFAOYSA-N
WJEOLQLKVOPQFV-UHFFFAOYSA-N…
计算化学: 氢键受体数7.0氢键供体数2.0可旋转键数7.0

物理性质

熔点90-95°C
沸点90-95°C
密度1.280±0.06 g/cm3(预测)
pKa:13.24±0.70(预测)
PSA:101.63
LogP:5.2786
折射率1.682
溶解性Chloroform (Slightly), Dichloromethane (Slightly), DMSO (Slightly), Methanol (Slightly)
外观形态类白色至浅米色固体
储存条件冰箱
产品应用该化合物用于治疗固态肿瘤.

MSDS等安全信息

GHS符号GHS07,GHS08
警示词Warning
危险描述H315-H319-H361-H335-H373
防范说明P201-P202-P260-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P308+P313-P312-P321-P314-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

上下游产品

2-[(2-Methyl-5-Tert-Butoxycarbonylaminophenyl)Amino]-4-(3-Pyridyl)Thiazole
2-(2-甲基-5-氨基苯基氨基)-4-(3-吡啶)噻唑 6-Methyl-N1-(4-(Pyridin-3-yl)Thiazol-2-yl)Benzene-1,3-Diamine 660837-08-1

合成工艺路线路线简述

合成目标产物 Masitinib 主要起始原料 4-Methyl-N3-(4-Pyridin-3-Yl-Thiazol-2-yl)-Benzene-1,3-Diamine And Methyl 4-[(4-Methylpiperazin-1-yl)Methyl]Benzoate
106261-64-7 + 660837-08-1 = 790299-79-5
反应条件:1.1 Reagents: Triethylamine Solvents: Dichloromethane,Tetrahydrofuran; 5 - 10 °C; 5 H,10 °C -> Rt
标题:Synthesis Of Masitinib
作者:Yang,Zhao; Wang,Zhixiang; Fang,Zheng; Bao,Shuxin; Guo,Kai
参考文献:Zhongguo Xiandai Yingyong Yaoxue 日期:2013 卷标:30(1) 页码:35-38

3-(2-溴乙酰基)吡啶氢溴酸盐置于三甲基铝,Potassium Hydrogencarbonate,三氟乙酸体系中,用乙醇,二氯甲烷,甲苯作为反应溶剂,化学反应 27.5H,反应生成马赛替尼
参考文献: Use Of C-Kit Inhibitors For Treating Type Ii Diabetes[fr] Utilisation D'Inhibiteurs De C-Kit Pour Le Traitement Du Diabete De Type Ii
标题: Use Of C-Kit Inhibitors For Treating Type Ii Diabetes[fr] Utilisation D'Inhibiteurs De C-Kit Pour Le Traitement Du Diabete De Type Ii

海关参考信息

2912110000-甲醛
2912210000-苯甲醛
2921211000-乙二胺
2933310010-吡啶
💡 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。
详情请参考：📖 海关编码查询和海关进出口税则

专利信息

专利号:US-2022233673-A1
优先权日:2019-06-04
标题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÃ‰DÃ‰RIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR Ã‰RIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:AU-2008214679-A1
优先权日:2007-02-13
标题 :Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors

专利号:US-2010121063-A1
优先权日:2007-02-13
标题:Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors

专利号:CA-2970628-A1
优先权日:2007-02-13
标题:Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors

专利号:US-8153792-B2
优先权日:2007-02-13
标题 :Process for the synthesis of 2-aminothiazole compounds as kinase inhibitors

专利号:BR-PI0807626-B1
优先权日:2007-02-13
标题 :PROCESS FOR THE SYNTHESIS OF 2-AMINOTHIAZOLE COMPOUNDS AS KINASE INHIBITORS

其他信息查阅

台州开创生物医药有限公司

网址: http://www.creatingbiopharm.com
企业联系电话：0576-88827176;18906581668👤
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主要参考文献

1: Kocic I, Kowianski P, Rusiecka I, Lietzau G, Mansfield C, Moussy A, Hermine O, Dubreuil P. Neuroprotective effect of masitinib in rats with postischemic stroke. Naunyn Schmiedebergs Arch Pharmacol. 2015 Jan;388(1):79-86. doi: 10.1007/s00210-014-1061-6. Epub 2014 Oct 26.
2: Adenis A, Blay JY, Bui-Nguyen B, BouchÃ© O, Bertucci F, Isambert N, Bompas E, Chaigneau L, Domont J, Ray-Coquard I, BlÃ©sius A, Van Tine BA, Bulusu VR, Dubreuil P, Mansfield CD, Acin Y, Moussy A, Hermine O, Le Cesne A. Masitinib in advanced gastrointestinal stromal tumor (GIST) after failure of imatinib: a randomized controlled open-label trial. Ann Oncol. 2014 Sep;25(9):1762-9. doi: 10.1093/annonc/mdu237. Epub 2014 Jul 25.
3: Rathore K, Alexander M, Cekanova M. Piroxicam inhibits Masitinib-induced cyclooxygenase 2 expression in oral squamous cell carcinoma cells in vitro. Transl Res. 2014 Aug;164(2):158-68. doi: 10.1016/j.trsl.2014.02.002. Epub 2014 Feb 21. doi: 10.3892/ijo.2014.2341. Epub 2014 Mar 13.

合成参考文献

参考文献:10.1007/s10406-007-0233-6
摘要:Lassau N, Chami L, Benatsou B, Peronneau P, Roche A. Dynamic contrast-enhanced ultrasonography (DCE-US) with quantification of tumor perfusion: a new diagnostic tool to evaluate the early effects of antiangiogenic treatment. Eur Radiol. 2007 Dec;17 Suppl 6():F89–98. doi: 10.1007/s10406-007-0233-6.
参考文献:10.1186/1746-6148-10-105
摘要:Halsey CH, Gustafson DL, Rose BJ, Wolf-Ringwall A, Burnett RC, Duval DL, Avery AC, Thamm DH. Development of an in vitro model of acquired resistance to toceranib phosphate (Palladia®) in canine mast cell tumor. BMC Veterinary Research. 2014 May 06;10(1):105. doi: 10.1186/1746-6148-10-105.
参考文献:10.3748/wjg.v21.i37.10493
摘要:Leporini C, Ammendola M, Marech I, Sammarco G, Sacco R, Gadaleta CD, Oakley C, Russo E, De Sarro G, Ranieri G. Targeting mast cells in gastric cancer with special reference to bone metastases. World J Gastroenterol. 2015 Oct 07;21(37):10493–501.
参考文献:10.1038/s41575-018-0005-x
摘要:Neoptolemos JP, Kleeff J, Michl P, Costello E, Greenhalf W, Palmer DH. Therapeutic developments in pancreatic cancer: current and future perspectives. Nature Reviews Gastroenterology & Hepatology. 2018 May 01;15(6):333–48. doi: 10.1038/s41575-018-0005-x.
参考文献:10.1007/s12016-019-08753-w
摘要:Komi DEA, Redegeld FA. Role of Mast Cells in Shaping the Tumor Microenvironment. Clinical Reviews in Allergy & Immunology. 2019 Jun 29;58(3):313–25. doi: 10.1007/s12016-019-08753-w.