PP242 (BioDeep_00000782146)
代谢物信息卡片
化学式: C16H16N6O (308.13855259999997)
中文名称: Torkinib
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)N1C2=NC=NC(=C2C(=N1)C3=CC4=C(N3)C=CC(=C4)O)N
InChI: InChI=1S/C16H16N6O/c1-8(2)22-16-13(15(17)18-7-19-16)14(21-22)12-6-9-5-10(23)3-4-11(9)20-12/h3-8,20,23H,1-2H3,(H2,17,18,19)
描述信息
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor > C61074 - Serine/Threonine Kinase Inhibitor
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C2201 - mTOR Inhibitor
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM[1]. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively[2].
Torkinib (PP 242) is a selective and ATP-competitive mTOR inhibitor with an IC50 of 8 nM[1]. PP242 inhibits both mTORC1 and mTORC2 with IC50s of 30 nM and 58 nM, respectively[2].
同义名列表
数据库引用编号
7 个数据库交叉引用编号
- ChEBI: CHEBI:95099
- ChEBI: CHEBI:90679
- PubChem: 135565635
- ChEMBL: CHEMBL1241674
- ChEMBL: CHEMBL3988893
- CAS: 1092351-67-1
- medchemexpress: HY-10474
分类词条
相关代谢途径
Reactome(0)
BioCyc(0)
PlantCyc(0)
代谢反应
0 个相关的代谢反应过程信息。
Reactome(0)
BioCyc(0)
WikiPathways(0)
Plant Reactome(0)
INOH(0)
PlantCyc(0)
COVID-19 Disease Map(0)
PathBank(0)
PharmGKB(0)
0 个相关的物种来源信息
在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有:
- PubMed: 来源于PubMed文献库中的文献信息,我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表,这个列表按照代谢物同时出现的文献数量降序排序,取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘,得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序,取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中,存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称,可以跳转到相关代谢物的信息页面。
文献列表
- Cuicui Sun, Xiaoyan Yang, Zhi Jin, Zuhua Gao. Combination of mTOR inhibitor PP242 and AMPK activator metformin exerts enhanced inhibitory effects on colorectal carcinoma cells in vitro by blocking multiple kinase pathways.
Journal of chemotherapy (Florence, Italy).
2022 Jun; ?(?):1-11. doi:
10.1080/1120009x.2022.2091122
. [PMID: 35731713] - Md Mamunur Rashid, Hyunbeom Lee, Byung Hwa Jung. Evaluation of the antitumor effects of PP242 in a colon cancer xenograft mouse model using comprehensive metabolomics and lipidomics.
Scientific reports.
2020 10; 10(1):17523. doi:
10.1038/s41598-020-73721-w
. [PMID: 33067464] - Xiaofang Tan, Huifeng Guan, Yang Yang, Shenying Luo, Lina Hou, Hongzhuan Chen, Juan Li. Cu(II) disrupts autophagy-mediated lysosomal degradation of oligomeric Aβ in microglia via mTOR-TFEB pathway.
Toxicology and applied pharmacology.
2020 08; 401(?):115090. doi:
10.1016/j.taap.2020.115090
. [PMID: 32512069] - Ritesh K Srivastava, Changzhao Li, Jasim Khan, Nilam Sanjib Banerjee, Louise T Chow, Mohammad Athar. Combined mTORC1/mTORC2 inhibition blocks growth and induces catastrophic macropinocytosis in cancer cells.
Proceedings of the National Academy of Sciences of the United States of America.
2019 12; 116(49):24583-24592. doi:
10.1073/pnas.1911393116
. [PMID: 31732667] - Denise Rageot, Thomas Bohnacker, Anna Melone, Jean-Baptiste Langlois, Chiara Borsari, Petra Hillmann, Alexander M Sele, Florent Beaufils, Marketa Zvelebil, Paul Hebeisen, Wolfgang Löscher, John Burke, Doriano Fabbro, Matthias P Wymann. Discovery and Preclinical Characterization of 5-[4,6-Bis({3-oxa-8-azabicyclo[3.2.1]octan-8-yl})-1,3,5-triazin-2-yl]-4-(difluoromethyl)pyridin-2-amine (PQR620), a Highly Potent and Selective mTORC1/2 Inhibitor for Cancer and Neurological Disorders.
Journal of medicinal chemistry.
2018 11; 61(22):10084-10105. doi:
10.1021/acs.jmedchem.8b01262
. [PMID: 30359003] - Hewei Zhang, Qinfang Liu, Weiwei Su, Jianke Wang, Yaru Sun, Junfeng Zhang, Ke Shang, Zhenhai Chen, Shipeng Cheng, Hua Wu. Genome-wide analysis of differentially expressed genes and the modulation of PEDV infection in Vero E6 cells.
Microbial pathogenesis.
2018 Apr; 117(?):247-254. doi:
10.1016/j.micpath.2018.02.004
. [PMID: 29408315] - Md Mamunur Rashid, Hyunbeom Lee, Byung Hwa Jung. Metabolite identification and pharmacokinetic profiling of PP242, an ATP-competitive inhibitor of mTOR using ultra high-performance liquid chromatography and mass spectrometry.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2018 Jan; 1072(?):244-251. doi:
10.1016/j.jchromb.2017.11.027
. [PMID: 29195143] - Kameswaran Ravichandran, Iram Zafar, Abdullah Ozkok, Charles L Edelstein. An mTOR kinase inhibitor slows disease progression in a rat model of polycystic kidney disease.
Nephrology, dialysis, transplantation : official publication of the European Dialysis and Transplant Association - European Renal Association.
2015 Jan; 30(1):45-53. doi:
10.1093/ndt/gfu296
. [PMID: 25239638] - Catherine E Gleason, Gustavo Frindt, Chih-Jen Cheng, Michael Ng, Atif Kidwai, Priyanka Rashmi, Florian Lang, Michel Baum, Lawrence G Palmer, David Pearce. mTORC2 regulates renal tubule sodium uptake by promoting ENaC activity.
The Journal of clinical investigation.
2015 Jan; 125(1):117-28. doi:
10.1172/jci73935
. [PMID: 25415435] - Tengis S Pavlov, Daria V Ilatovskaya, Vladislav Levchenko, Lijun Li, Carolyn M Ecelbarger, Alexander Staruschenko. Regulation of ENaC in mice lacking renal insulin receptors in the collecting duct.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology.
2013 Jul; 27(7):2723-32. doi:
10.1096/fj.12-223792
. [PMID: 23558339] - Haiyan Li, Jun Lin, Xiaokai Wang, Guangyu Yao, Liping Wang, Hang Zheng, Cuilan Yang, Chunhong Jia, Anling Liu, Xiaochun Bai. Targeting of mTORC2 prevents cell migration and promotes apoptosis in breast cancer.
Breast cancer research and treatment.
2012 Aug; 134(3):1057-66. doi:
10.1007/s10549-012-2036-2
. [PMID: 22476852] - Qingsong Liu, Jinhua Wang, Seong A Kang, Carson C Thoreen, Wooyoung Hur, Tausif Ahmed, David M Sabatini, Nathanael S Gray. Discovery of 9-(6-aminopyridin-3-yl)-1-(3-(trifluoromethyl)phenyl)benzo[h][1,6]naphthyridin-2(1H)-one (Torin2) as a potent, selective, and orally available mammalian target of rapamycin (mTOR) inhibitor for treatment of cancer.
Journal of medicinal chemistry.
2011 Mar; 54(5):1473-80. doi:
10.1021/jm101520v
. [PMID: 21322566]