CAS: 1138549-36-6; 2-(4-Methyl-1,4-Diazepan-1-yl)-N-((5-Methylpyrazin-2-yl)Methyl)-5-Oxo-5H-Benzo[4,5]Thiazolo[3,2-A][1,8]Naphthyridine-6-Carboxamide

上下游产品

ethyl 2-(4-methyl-1,4-diazepan-1-yl)-5-oxo-5H-benzo[4,5]thiazolo-[3,2-a][1,8]-naphthyridine-6-carboxylate (5-methylpyrazine-2-yl)methylamine ethyl 2-chloro-5-oxo-5H-benzo[4,5]thiazolo[3,2-a][1,8]naphthyridine-6-carboxylate 2,6-dichloropyridine-3-carboxylic acid

📜Ethyl 2-Chloro-5-Oxo-5H-Benzo[4,5]Thiazolo[3,2-A][1,8]Naphthyridine-6-Carboxylate置于aluminum (III) Chloride,1,8-二氮杂双环[5.4.0]十一碳-7-烯体系中,用 二氯甲烷,乙腈 用作溶剂,化学反应 5.5H,反应生成2-(4-甲基-1H-1,4-二氮杂环庚烷-1-基)-N-[(5-甲基-2-吡嗪基)甲基]-5-氧代-5H-苯并噻唑并[3,2-A][1,8]萘啶-6-甲酰胺
参考文献:Discovery Of Cx-5461,The First Direct And Selective Inhibitor Of Rna Polymerase I,For Cancer Therapeutics
标题:Discovery Of Cx-5461,The First Direct And Selective Inhibitor Of Rna Polymerase I,For Cancer Therapeutics
摘要:Accelerated Proliferation Of Solid Tumor And Hematologic Cancer Cells Is Linked To Accelerated Transcription Of Rdna By The Rna Polymerase I (Pol I) Enzyme To Produce Elevated Levels Of Rrna (Rrna). Indeed,Upregulation Of Pol I,Frequently Caused By Mutational Alterations Among Tumor Suppressors And Oncogenes,Is Required For Maintenance Of The Cancer Phenotype And Forms The Basis For Seeking Selective Inhibitors Of Pot I As Anticancer Therapeutics. 2-(4-Methyl-[1,4]Diazepan-1-yl)-5-Oxo-5H-7-Thia-1,11B-Diaza-Benzo[c]Fluorene-6-Carboxylic Acid (5-Methyl-Pyrazin-2-Ylmethyl)-Amide (Cx-5461,7C) Has Been Identified As The First Potent,Selective,And Orally Bioavailable Inhibitor Of Rna Pot I Transcription With In Vivo Activity In Tumor Growth Efficacy Models. The Preclinical Data Support The Development Of Cx-5461 As An Anticancer Drug With Potential For Activity In Several Types Of Cancer.
Doi:10.1021/ml300110S

专利信息

专利号:US-2025084447-A1
优先权日:2023-09-07
标 题 :METHOD FOR PREPARING STABLE ISOTOPE-LABELED ssDNA BY BIOSYNTHESIS WITH ESCHERICHIA COLI
发明人：WANG SHENLIN; ZOU MENGBING; MA CHANGXING
权利人:UNIV EAST CHINA SCIENCE & TECH
摘要:Provided is a method for preparing stable isotope-labeled single-stranded DNA (ssDNA) by biosynthesis with E. coli, and the 15NH4Cl or 13C-Glcose is used as the only nitrogen or carbon source, which may significantly reduce costs. In the method of the present disclosure, the target sequence of ssDNA is tandemly duplicated on a high-copy vector, a site for a first restriction endonuclease and a site for a second restriction endonuclease are added to the 5′ and 3′ ends of the target sequence, respectively, and the recombinant vector is digested to obtain an asymmetric double-stranded DNA structure, which is then isolated by denaturation to obtain two ssDNAs of unequal lengths, including 15N- or 13C-labeled target ssDNA. The method of the present disclosure is able to effectively increase the yield of ssDNA, thereby improving the efficiency of in vitro synthesis of isotope labeled ssDNA.

专利号:US-2023160018-A1
优先权日:2020-04-16
标 题 :Crybetab2 predicts poor breast cancer outcome and sensitizes tumors to nucleolin and cdk inhibition
发明人：MERINO VANESSA FERREIRA; POMPER MARTIN; SUKUMAR SARASWATI
权利人:UNIV JOHNS HOPKINS
摘要:CKYPB2 induces EMT, sternness, protein synthesis and cell cycle progression through regulation of nucleolin, con-tributing to an increase in tumor growth and metastasis. CKYPB2 can be used as a prognostic marker in African American women with TNBC. CKYPB2 can further select patients with TNBC and ER positive tumors that will likely benefit from inhibitors of ribosomal RNA synthesis, CDK4 and nucleolin.