PI-103 (BioDeep_00000605723)

   


代谢物信息卡片


3-[4-(4-morpholinyl)pyrido[3,2:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol

化学式: C19H16N4O3 (348.12223459999996)
中文名称: PI-103 抑制剂
谱图信息: 最多检出来源 () 0%

分子结构信息

SMILES: C1COCCN1C2=NC(=NC3=C2OC4=C3C=CC=N4)C5=CC(=CC=C5)O
InChI: InChI=1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2

描述信息

PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy[1][2][3][4].
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy[1][2][3][4].

同义名列表

2 个代谢物同义名

PI-103; 3-[4-(4-morpholinyl)pyrido[3,2:4,5]furo[3,2-d]pyrimidin-2-yl]-phenol



数据库引用编号

6 个数据库交叉引用编号

分类词条

相关代谢途径

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代谢反应

0 个相关的代谢反应过程信息。

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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

  • Rosalin Mishra, Long Yuan, Hima Patel, Aniruddha S Karve, Haizhou Zhu, Aaron White, Samar Alanazi, Pankaj Desai, Edward J Merino, Joan T Garrett. Phosphoinositide 3-Kinase (PI3K) Reactive Oxygen Species (ROS)-Activated Prodrug in Combination with Anthracycline Impairs PI3K Signaling, Increases DNA Damage Response and Reduces Breast Cancer Cell Growth. International journal of molecular sciences. 2021 Feb; 22(4):. doi: 10.3390/ijms22042088. [PMID: 33669867]
  • Zhen Xiao, Cilong Chu, Lingjia Zhou, Zhihui Zhou, Qian Zhang, Feiyi Yang, Zunhua Yang, Pengwu Zheng, Shan Xu, Wufu Zhu. Discovery of thiapyran-pyrimidine derivatives as potential EGFR inhibitors. Bioorganic & medicinal chemistry. 2020 10; 28(19):115669. doi: 10.1016/j.bmc.2020.115669. [PMID: 32912435]
  • Lan Luo, Qiu Zhong, Shanchun Guo, Changde Zhang, Qiang Zhang, Shilong Zheng, Ling He, Guangdi Wang. Development of a bioavailable boron-containing PI-103 Bioisostere, PI-103BE. Bioorganic & medicinal chemistry letters. 2020 07; 30(14):127258. doi: 10.1016/j.bmcl.2020.127258. [PMID: 32527558]
  • Ya'nan Yu, Yuqiao Han, Fupo Zhang, Zhenmei Gao, Tong Zhu, Suzhen Dong, Mingliang Ma. Design, Synthesis, and Biological Evaluation of Imidazo[1,2-a]pyridine Derivatives as Novel PI3K/mTOR Dual Inhibitors. Journal of medicinal chemistry. 2020 03; 63(6):3028-3046. doi: 10.1021/acs.jmedchem.9b01736. [PMID: 32069401]
  • Xiaodong Ma, Jun Wei, Chang Wang, Dongyan Gu, Yongzhou Hu, Rong Sheng. Design, synthesis and biological evaluation of novel benzothiadiazine derivatives as potent PI3Kδ-selective inhibitors for treating B-cell-mediated malignancies. European journal of medicinal chemistry. 2019 May; 170(?):112-125. doi: 10.1016/j.ejmech.2019.03.005. [PMID: 30878826]
  • Cholpon S Djuzenova, Vanessa Fiedler, Simon Memmel, Astrid Katzer, Dmitri Sisario, Philippa K Brosch, Alexander Göhrung, Svenja Frister, Heiko Zimmermann, Michael Flentje, Vladimir L Sukhorukov. Differential effects of the Akt inhibitor MK-2206 on migration and radiation sensitivity of glioblastoma cells. BMC cancer. 2019 Apr; 19(1):299. doi: 10.1186/s12885-019-5517-4. [PMID: 30943918]
  • Hui Wang, Yujian Zhang, Yongning Lu, Jiajia Song, Min Huang, Jin Zhang, Yiran Huang. The role of stearoyl-coenzyme A desaturase 1 in clear cell renal cell carcinoma. Tumour biology : the journal of the International Society for Oncodevelopmental Biology and Medicine. 2016 Jan; 37(1):479-89. doi: 10.1007/s13277-015-3451-x. [PMID: 26224474]
  • Gigin Lin, Gabriela Andrejeva, Anne-Christine Wong Te Fong, Deborah K Hill, Matthew R Orton, Harry G Parkes, Dow-Mu Koh, Simon P Robinson, Martin O Leach, Thomas R Eykyn, Yuen-Li Chung. Reduced Warburg effect in cancer cells undergoing autophagy: steady- state 1H-MRS and real-time hyperpolarized 13C-MRS studies. PloS one. 2014; 9(3):e92645. doi: 10.1371/journal.pone.0092645. [PMID: 24667972]
  • Ben A Hall, Tae Yeon Kim, Maxwell N Skor, Suzanne D Conzen. Serum and glucocorticoid-regulated kinase 1 (SGK1) activation in breast cancer: requirement for mTORC1 activity associates with ER-alpha expression. Breast cancer research and treatment. 2012 Sep; 135(2):469-79. doi: 10.1007/s10549-012-2161-y. [PMID: 22842983]
  • Teresa Fernández-Acero, Isabel Rodríguez-Escudero, Francisca Vicente, Maria Cândida Monteiro, José R Tormo, Juan Cantizani, María Molina, Víctor J Cid. A yeast-based in vivo bioassay to screen for class I phosphatidylinositol 3-kinase specific inhibitors. Journal of biomolecular screening. 2012 Sep; 17(8):1018-29. doi: 10.1177/1087057112450051. [PMID: 22706348]
  • Giovanna Bergamini, Kathryn Bell, Satoko Shimamura, Thilo Werner, Andrew Cansfield, Katrin Müller, Jessica Perrin, Christina Rau, Katie Ellard, Carsten Hopf, Carola Doce, Daniel Leggate, Raffaella Mangano, Toby Mathieson, Alison O'Mahony, Ivan Plavec, Faiza Rharbaoui, Friedrich Reinhard, Mikhail M Savitski, Nigel Ramsden, Emilio Hirsch, Gerard Drewes, Oliver Rausch, Marcus Bantscheff, Gitte Neubauer. A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. Nature chemical biology. 2012 Apr; 8(6):576-82. doi: 10.1038/nchembio.957. [PMID: 22544264]
  • Kyota Aoyagi, Mica Ohara-Imaizumi, Chiyono Nishiwaki, Yoko Nakamichi, Kohjiro Ueki, Takashi Kadowaki, Shinya Nagamatsu. Acute inhibition of PI3K-PDK1-Akt pathway potentiates insulin secretion through upregulation of newcomer granule fusions in pancreatic β-cells. PloS one. 2012; 7(10):e47381. doi: 10.1371/journal.pone.0047381. [PMID: 23077605]
  • Minoru Ito, Michiaki Nagasawa, Naoki Omae, Tomohiro Ide, Yunike Akasaka, Koji Murakami. Differential regulation of CIDEA and CIDEC expression by insulin via Akt1/2- and JNK2-dependent pathways in human adipocytes. Journal of lipid research. 2011 Aug; 52(8):1450-60. doi: 10.1194/jlr.m012427. [PMID: 21636835]
  • Morag K Mansley, Stuart M Wilson. Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. British journal of pharmacology. 2010 Oct; 161(3):571-88. doi: 10.1111/j.1476-5381.2010.00898.x. [PMID: 20880397]
  • Nada M S Al-Saffar, L Elizabeth Jackson, Florence I Raynaud, Paul A Clarke, Ana Ramírez de Molina, Juan C Lacal, Paul Workman, Martin O Leach. The phosphoinositide 3-kinase inhibitor PI-103 downregulates choline kinase alpha leading to phosphocholine and total choline decrease detected by magnetic resonance spectroscopy. Cancer research. 2010 Jul; 70(13):5507-17. doi: 10.1158/0008-5472.can-09-4476. [PMID: 20551061]
  • Simon Miller, Brandon Tavshanjian, Arkadiusz Oleksy, Olga Perisic, Benjamin T Houseman, Kevan M Shokat, Roger L Williams. Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34. Science (New York, N.Y.). 2010 Mar; 327(5973):1638-42. doi: 10.1126/science.1184429. [PMID: 20339072]
  • Paul Workman, Paul A Clarke, Florence I Raynaud, Rob L M van Montfort. Drugging the PI3 kinome: from chemical tools to drugs in the clinic. Cancer research. 2010 Mar; 70(6):2146-57. doi: 10.1158/0008-5472.can-09-4355. [PMID: 20179189]
  • Swarajit K Biswas, Yan Zhao, Arumugam Nagalingam, Thomas W Gardner, Lakshman Sandirasegarane. PDGF- and insulin/IGF-1-specific distinct modes of class IA PI 3-kinase activation in normal rat retinas and RGC-5 retinal ganglion cells. Investigative ophthalmology & visual science. 2008 Aug; 49(8):3687-98. doi: 10.1167/iovs.07-1455. [PMID: 18421086]
  • Florence I Raynaud, Suzanne Eccles, Paul A Clarke, Angela Hayes, Bernard Nutley, Sonia Alix, Alan Henley, Francesca Di-Stefano, Zahida Ahmad, Sandrine Guillard, Lynn M Bjerke, Lloyd Kelland, Melanie Valenti, Lisa Patterson, Sharon Gowan, Alexis de Haven Brandon, Masahiko Hayakawa, Hiroyuki Kaizawa, Tomonubu Koizumi, Takahide Ohishi, Sonal Patel, Nahid Saghir, Peter Parker, Mike Waterfield, Paul Workman. Pharmacologic characterization of a potent inhibitor of class I phosphatidylinositide 3-kinases. Cancer research. 2007 Jun; 67(12):5840-50. doi: 10.1158/0008-5472.can-06-4615. [PMID: 17575152]
  • Qi-Wen Fan, Zachary A Knight, David D Goldenberg, Wei Yu, Keith E Mostov, David Stokoe, Kevan M Shokat, William A Weiss. A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. Cancer cell. 2006 May; 9(5):341-9. doi: 10.1016/j.ccr.2006.03.029. [PMID: 16697955]