CAS: 1213269-23-8; N-(3-((5-Chloro-2-((2-Methoxy-4-(4-Methylpiperazin-1-yl)Phenyl)Amino)Pyrimidin-4-yl)Oxy)Phenyl)Acrylamide

上下游产品

CAS号1213269-26-1 4-(3-氨基苯氧基)-5-氯... | CAS号814-68-6 丙烯酰氯 | CAS号122833-04-9 2-甲氧基-4-(4-甲基哌嗪... | CAS号76661-24-0 2,5-二氯-4-(3-硝基苯氧基)嘧啶 | CAS号554-84-7 3-硝基苯酚 | CAS号1213269-25-0 5-chloro-N-(2-m... | CAS号446-36-6 5-氟-2-硝基苯酚 | CAS号448-19-1 5-氟-2-硝基苯甲醚

N-甲基哌嗪置于palladium 10% On Activated Carbon,氢气,铁粉,Potassium Carbonate,氯化铵,N,N-二异丙基乙胺,三氟乙酸体系中,用 四氢呋喃,乙醇,二氯甲烷,水,N,N-二甲基甲酰胺,仲丁醇 用作溶剂,化学反应 10.0H,反应生成Wz 4002; N-[3-[[5-氯-2-[[2-甲氧基-4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氧基]苯基]-2-丙烯酰胺
参考文献:Wz4002类似物作为egfr抑制剂的设计,合成和生物学评估
标题:Wz4002类似物作为egfr抑制剂的设计,合成和生物学评估
摘要:合成了一系列来自wz4002的32个苯胺嘧啶,并使用lanthascreen结合测定法(egfr D746-750)或z'Lyte测定法(egfr-Wt,Egfr D746-750,Egfr)评价了六种不同egfr激酶的抑制百分比t790M,Egfr T790M L858R,Egfr C797S和egfr T790M L858R C797S).邻羟基乙酰胺10显示出所有六个激酶的完全抑制在10μm.对三突变体,Egfr T790M C797S L858R,化合物9-12在10 µm时表现出完全抑制,在1 µm时表现出几乎完全抑制.还使用mtt分析法评估了目标化合物,以确定其对人非小细胞肺癌细胞(pc9,Pc9Gr和h460)和小鼠白血病细胞(ba / F3 Wt和ba / F3T 3151)的细胞毒活性.总体而言,7,9-12,30和31被认为是在所有五种细胞系的最有效的化合物.
Doi:10.1016/j.Bmcl.2017.09.048

专利信息

专利号:US-11406709-B2
优先权日:2014-09-15
标 题 :Therapeutic and research application of PDCL3
发明人：RAHIMI NADER
权利人:UNIV BOSTON
摘要:Described herein are novel compositions comprising, for example, PDCL3 polypeptides having VEGFR-2 inhibitory activity, inhibitory PDCL3 antibodies and PDCL3-binding fragments thereof, or PDCL3 inhibitory nucleic acid molecules, and methods of their use in anti-angiogenesis and anti-tumor proliferation and invasiveness therapies, such as the treatment of cancer, as well as the treatment of those vascular diseases where pathological angiogenesis plays a role, such as in carotid artery disease, macular degeneration, and plaque neovascularization. Also described herein are novel compositions comprising engineered PDCL3 polypeptides having enhanced chaperone activity, recombinant cells comprising such engineered PDCL3 polypeptides having enhanced chaperone activity, and methods thereof for therapeutic protein production and in vitro protein synthesis.

专利号:US-2022396794-A1
优先权日:2019-06-04
标题:APTAMERS AGAINST TRANSFERRIN RECEPTOR (TfR)
发明人：HABIB NAGY; ROSSI JOHN; YOON SORAH; SWIDERSK PIOTR MAREK
权利人:APTERNA LTD; HOPE CITY
摘要:Methods of treating or preventing a disease or disorder are disclosed comprising administering to a subject in need thereof an effective amount of a nucleic acid compound comprising, or consisting of, a nucleic acid sequence capable of binding to a transferrin receptor (TfR) and an effective amount of an inhibitor of DNA synthesis. Also disclosed is a nucleic acid compound comprising, or consisting of, a nucleic acid sequence having at least 85% sequence identity to SEQ ID NO: 1, wherein said nucleic acid sequence is at least 30 nucleotides in length and at most 50 nucleotides in length, and wherein the nucleic acid sequence is capable of binding to a transferrin receptor (TfR).