CAS: 1353859-00-3; (E)-5-Chloro-3-((5-(3-(4-Methyl-1,4-Diazepane-1-Carbonyl)Phenyl)Furan-2-yl)Methylene)Indolin-2-One Hydrochloride
该化合物是PIM kinase家族的一种强力和选择性抑制剂,对PIM-1,PIM-2和PIM-3等效体表现出高度亲近性,这种小分子化合物通过干扰细胞生存和生长的关键信号路径,在各种癌症细胞线中表现出强烈的抗扩散活动;盐酸盐形式增加了溶解性和生物利用率,使之适合体外和体外研究应用;CX-6258盐酸盐在临床前研究中广泛用于调查PIM在肿瘤学和皮肤恶性方面依赖PIM的细胞性机制;该化合物的特征是其定义明确的药用植物基因特征和强效抑制作用,支持其作为针对动量研究的宝贵工具.
- 英文名称(E)-5-Chloro-3-((5-(3-(4-Methyl-1,4-Diazepane-1-Carbonyl)Phenyl)Furan-2-yl)Methylene)Indolin-2-One Hydrochloride
- 中文名称化合物CX-6258HCL
- IUPAC名称(E)-5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one hydrochloride
- 其它别名(3E)-5-Chloro-3-[[5-[3-[(Hexahydro-4-Methyl-1H-1,4-Diazepin-1-yl)Carbonyl]Phenyl]-2-Furanyl]Methylene]-1,3-Dihydro-2H-Indol-2-One, Hydrochloride (1:1); Pim-Kinase Inhibitor X; (E)-5-Chloro-3-((5-(3-(4-Methyl-1,4-Diazepane-1-Carbonyl)Phenyl)Furan-2-yl)Methylene)Indolin-2-One Hydrochloride
- CAS编号1353859-00-3
- MFCD编号:MFCD28137787
- 分子式:C26H25Cl2N3O3分子量:498.41
- 产品CID: 542668
- 同类组份化合物CAS1202916-90-2 (free base)1353858-99-7 (HCl hydrate)1353859-00-3 (HCl)
- 产品分类有机原料 → 有机杂环化合物 → 吲哚及其衍生物
物理性质
- PSA:65.79
- LogP:5.6862
- 溶解性DMSO:57.0(Max Conc. mg/mL);114.37(Max Conc. Mm) Ethanol:1.0(Max Conc. mg/mL);2.01(Max Conc. Mm)
- 外观形态橙色至红色固体
- 储存条件惰性气氛,室温
- 产品应用该化合物是一种强效的,口服的PIM-PIM 脂酶抑制剂,对PIM1,PIM2,PIM2和PIM3分别具有5纳米,25纳米和16纳米的IC50值;对一组人类癌症细胞线(IC50:0.02-3.7微克M)表现出抗生素性活性,在急性白血病细胞线中表现出最高敏感性;当与 DOXORUBICIN(10:1 摩尔比)或PALITAXEL(100:1 毫拉比)结合时,它显示出协同的细胞毒性,而综合指数(CI50)和16尼米;它以剂量为主的抑制皮肤蛋白质坏(在PIMS KINASE特定地点S112)和4E-BP1(在S65和T37/46);在活活生物中,它显示在抑制MV-4-11-XENOGRAFT鼠模型中肿瘤生长的剂量依赖性效果,在50毫克/千克和75%TGI/千克时达到45%的肿瘤生长抑制(TGIS).
上下游产品
5-(3-carboxyphenyl)furane-2-carbaldehyde 5-chloro-indolin-2-one (E)-3-(5-((5-chloro-2-oxoindolin-3-ylidene)methyl)furan-2-yl)benzoic acid (E)-(5-chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one)合成工艺路线路线简述
📜5-氯氧化吲哚置于哌啶,盐酸,N,N'-羰基二咪唑体系中,用 1,4-二氧六环,甲醇,乙醇,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 51.5H,反应生成化合物cx-6258Hcl
参考文献:Discovery Of Cx-6258. A Potent,Selective,And Orally Efficacious Pan-Pim Kinases Inhibitor
标题:Discovery Of Cx-6258. A Potent,Selective,And Orally Efficacious Pan-Pim Kinases Inhibitor
摘要:Structure Activity Relationship Analysis In A Series Of 3-(5-((2-Oxoindolin-3-Ylidene)Methyl)Furan-2-yl)Amides Identified Compound 13,A Pan-Pim Kinases Inhibitor With Excellent Biochemical Potency And Kinase Selectivity. Compound 13 Exhibited In Vitro Synergy With Chemotherapeutics And Robust In Vivo Efficacy In Two Pim Kinases Driven Tumor Models.
Doi:10.1021/ml200259Q
海关参考信息
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📌 第三方产品分析报告
主要参考文献
1: Fujii S, Nakamura S, Oda A, Miki H, Tenshin H, Teramachi J, Hiasa M, Bat-Erdene A, Maeda Y, Oura M, Takahashi M, Iwasa M, Endo I, Yoshida S, Aihara KI, Kurahashi K, Harada T, Kagawa K, Nakao M, Sano S, Abe M. Unique anti-myeloma activity by thiazolidine-2,4-dione compounds with Pim inhibiting activity. Br J Haematol. 2018 Jan;180(2):246-258. doi: 10.1111/bjh.15033. doi: 10.1038/s41598-017-13557-z.
3: Peterson BG, Tan KW, Osa-Andrews B, Iram SH. High-content screening of clinically tested anticancer drugs identifies novel inhibitors of human MRP1 (ABCC1). Pharmacol Res. 2017 May;119:313-326. doi: 10.1016/j.phrs.2017.02.024. Epub 2017 Feb 28. doi: 10.1158/1078-0432.CCR-16-0124. Epub 2016 Aug 2. doi: 10.1016/j.bmcl.2015.07.061. Epub 2015 Jul 26. doi: 10.1002/jcb.24444. doi: 10.1021/ml200259q. eCollection 2012 Feb 9.
合成参考文献
合成方法参考DOI号:10.1021/ml200259q
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