PD0325901 (BioDeep_00000837781)
代谢物信息卡片
化学式: C16H14F3IN2O4 (481.995039)
中文名称: N-[(2R)-2,3-二羟基丙氧基]-3,4-二氟-2-[(2-氟-4-碘苯)氨基]苯甲酰胺
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: C1=CC(=C(C=C1I)F)NC2=C(C=CC(=C2F)F)C(=O)NOCC(CO)O
InChI: InChI=1S/C16H14F3IN2O4/c17-11-3-2-10(16(25)22-26-7-9(24)6-23)15(14(11)19)21-13-4-1-8(20)5-12(13)18/h1-5,9,21,23-24H,6-7H2,(H,22,25)/t9-/m1/s1
描述信息
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C69145 - Mitogen-Activated Protein Kinase Kinase Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor
Mirdametinib (PD0325901) is an orally active, selective and non-ATP-competitive MEK inhibitor with an IC50 of 0.33 nM. Mirdametinib exhibits a Kiapp of 1 nM against activated MEK1 and MEK2. Mirdametinib suppresses the expression of p-ERK1/2 and induces apoptosis. Mirdametinib has anti-cancer activity for a broad spectrum of human tumor xenografts[1][2][3].
同义名列表
数据库引用编号
8 个数据库交叉引用编号
- ChEBI: CHEBI:88249
- KEGGdrug: D11675
- PubChem: 9826528
- DrugBank: DB07101
- ChEMBL: CHEMBL507361
- CAS: 391209-97-5
- CAS: 391210-10-9
- medchemexpress: HY-10254
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
- Zhao Yang, Xuming Yang, Mingchun An. Polyphyllin I improves myocardial damage in coronary artery disease via modulating lipid metabolism and myocardial apoptosis.
Journal of biochemical and molecular toxicology.
2022 Dec; 36(12):e23219. doi:
10.1002/jbt.23219
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Journal of medicinal chemistry.
2020 12; 63(24):15883-15905. doi:
10.1021/acs.jmedchem.0c01609
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Cell death & disease.
2020 08; 11(8):617. doi:
10.1038/s41419-020-02845-8
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Scientific reports.
2018 11; 8(1):16170. doi:
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. [PMID: 30385793] - Cuiping Li, Weiyi Lai, Hailin Wang. An Alternative Culture Method to Maintain Genomic Hypomethylation of Mouse Embryonic Stem Cells Using MEK Inhibitor PD0325901 and Vitamin C.
Journal of visualized experiments : JoVE.
2018 06; ?(136):. doi:
10.3791/56391
. [PMID: 29912180] - Matthew A Summers, Emily R Vasiljevski, Kathy Mikulec, Lauren Peacock, David G Little, Aaron Schindeler. Developmental dosing with a MEK inhibitor (PD0325901) rescues myopathic features of the muscle-specific but not limb-specific Nf1 knockout mouse.
Molecular genetics and metabolism.
2018 04; 123(4):518-525. doi:
10.1016/j.ymgme.2018.02.009
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Targeted oncology.
2017 Dec; 12(6):775-785. doi:
10.1007/s11523-017-0530-5
. [PMID: 29067643] - C Marcela Diaz-Montero, Frances J Mao, John Barnard, Yvonne Parker, Maryam Zamanian-Daryoush, John J Pink, James H Finke, Brian I Rini, Daniel J Lindner. MEK inhibition abrogates sunitinib resistance in a renal cell carcinoma patient-derived xenograft model.
British journal of cancer.
2016 10; 115(8):920-928. doi:
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2016 10; 30(10):3489-3500. doi:
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Stem cell reports.
2016 05; 6(5):717-728. doi:
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. [PMID: 27132887] - Xueying Luo, Binlong Zhong, Xian Hong, Yurong Cui, Ying Gao, Mengmeng Yin, Ming Tang, Jürgen Hescheler, Jiaoya Xi. Puerarin Exerts a Delayed Inhibitory Effect on the Proliferation of Cardiomyocytes Derived from Murine ES Cells via Slowing Progression through G2/M Phase.
Cellular physiology and biochemistry : international journal of experimental cellular physiology, biochemistry, and pharmacology.
2016; 38(4):1333-42. doi:
10.1159/000443077
. [PMID: 27008508] - Vaibhav Sidarala, Rajakrishnan Veluthakal, Khadija Syeda, Anjaneyulu Kowluru. EHT 1864, a small molecule inhibitor of Ras-related C3 botulinum toxin substrate 1 (Rac1), attenuates glucose-stimulated insulin secretion in pancreatic β-cells.
Cellular signalling.
2015 Jun; 27(6):1159-67. doi:
10.1016/j.cellsig.2015.02.020
. [PMID: 25725286] - Bas Brinkhof, Helena T A van Tol, Marian J A Groot Koerkamp, Frank M Riemers, Sascha G IJzer, Kaveh Mashayekhi, Henk P Haagsman, Bernard A J Roelen. A mRNA landscape of bovine embryos after standard and MAPK-inhibited culture conditions: a comparative analysis.
BMC genomics.
2015 Apr; 16(?):277. doi:
10.1186/s12864-015-1448-x
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Cellular signalling.
2015 Mar; 27(3):545-54. doi:
10.1016/j.cellsig.2014.12.017
. [PMID: 25562429] - Mehdi Pirouz, Ali Rahjouei, Farnaz Shamsi, Kolja Neil Eckermann, Gabriela Salinas-Riester, Claudia Pommerenke, Michael Kessel. Destabilization of pluripotency in the absence of Mad2l2.
Cell cycle (Georgetown, Tex.).
2015; 14(10):1596-610. doi:
10.1080/15384101.2015.1026485
. [PMID: 25928475] - Joao A Paulo, Fiona E McAllister, Robert A Everley, Sean A Beausoleil, Alexander S Banks, Steven P Gygi. Effects of MEK inhibitors GSK1120212 and PD0325901 in vivo using 10-plex quantitative proteomics and phosphoproteomics.
Proteomics.
2015 Jan; 15(2-3):462-73. doi:
10.1002/pmic.201400154
. [PMID: 25195567] - Farnoosh Attari, Houri Sepehri, Hassan Ansari, Seyedeh-Nafiseh Hassani, Fereshteh Esfandiari, Behrouz Asgari, Abdolhossein Shahverdi, Hossein Baharvand. Efficient induction of pluripotency in primordial germ cells by dual inhibition of TGF-β and ERK signaling pathways.
Stem cells and development.
2014 May; 23(10):1050-61. doi:
10.1089/scd.2013.0438
. [PMID: 24382167] - Daofang Ding, Linghui Li, Yi Song, Guoqing DU, Xiaoen Wei, Yuelong Cao. [MAPK-ERK1/2 signaling pathway regulates osteogenic gene expression in rat osteoblasts in vitro].
Nan fang yi ke da xue xue bao = Journal of Southern Medical University.
2013 Oct; 33(10):1432-6. doi:
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. [PMID: 24144741] - Ingo V Hartung, Marion Hitchcock, Florian Pühler, Roland Neuhaus, Arne Scholz, Stefanie Hammer, Kirstin Petersen, Gerhard Siemeister, Dominic Brittain, Roman C Hillig. Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories.
Bioorganic & medicinal chemistry letters.
2013 Apr; 23(8):2384-90. doi:
10.1016/j.bmcl.2013.02.028
. [PMID: 23474388] - Martin Y H Zhang, Daniel Ranch, Renata C Pereira, Harvey J Armbrecht, Anthony A Portale, Farzana Perwad. Chronic inhibition of ERK1/2 signaling improves disordered bone and mineral metabolism in hypophosphatemic (Hyp) mice.
Endocrinology.
2012 Apr; 153(4):1806-16. doi:
10.1210/en.2011-1831
. [PMID: 22334725] - Ta-Chun Hang, Douglas A Lauffenburger, Linda G Griffith, Donna B Stolz. Lipids promote survival, proliferation, and maintenance of differentiation of rat liver sinusoidal endothelial cells in vitro.
American journal of physiology. Gastrointestinal and liver physiology.
2012 Feb; 302(3):G375-88. doi:
10.1152/ajpgi.00288.2011
. [PMID: 22075778] - Dolores Diaz, Krishna Allamneni, Jacqueline M Tarrant, Sock-Cheng Lewin-Koh, Rama Pai, Preeti Dhawan, Gary R Cain, Cleopatra Kozlowski, Hajime Hiraragi, Nghi La, Dylan P Hartley, Xiao Ding, Brian J Dean, Sheila Bheddah, Donna M Dambach. Phosphorous dysregulation induced by MEK small molecule inhibitors in the rat involves blockade of FGF-23 signaling in the kidney.
Toxicological sciences : an official journal of the Society of Toxicology.
2012 Jan; 125(1):187-95. doi:
10.1093/toxsci/kfr263
. [PMID: 21976371] - Maitham A Khajah, Sanaa Al Saleh, Princy M Mathew, Yunus A Luqmani. Differential effect of growth factors on invasion and proliferation of endocrine resistant breast cancer cells.
PloS one.
2012; 7(7):e41847. doi:
10.1371/journal.pone.0041847
. [PMID: 22860018] - Seung Hee Kang, Hee-Jeong Cho, Gayong Shim, Sangbin Lee, Su-Hyeon Kim, Han-Gon Choi, Chan-Wha Kim, Yu-Kyoung Oh. Cationic liposomal co-delivery of small interfering RNA and a MEK inhibitor for enhanced anticancer efficacy.
Pharmaceutical research.
2011 Dec; 28(12):3069-78. doi:
10.1007/s11095-011-0569-4
. [PMID: 21879387] - Nan Cao, Jing Liao, Zumei Liu, Wenmin Zhu, Jia Wang, Lijun Liu, Lili Yu, Ping Xu, Chun Cui, Lei Xiao, Huang-Tian Yang. In vitro differentiation of rat embryonic stem cells into functional cardiomyocytes.
Cell research.
2011 Sep; 21(9):1316-31. doi:
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. [PMID: 21423272] - Daniel Ranch, Martin Yh Zhang, Anthony A Portale, Farzana Perwad. Fibroblast growth factor 23 regulates renal 1,25-dihydroxyvitamin D and phosphate metabolism via the MAP kinase signaling pathway in Hyp mice.
Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research.
2011 Aug; 26(8):1883-90. doi:
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PloS one.
2010 Nov; 5(11):e15518. doi:
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. [PMID: 21124737] - Ying C Henderson, Yunyun Chen, Mitchell J Frederick, Stephen Y Lai, Gary L Clayman. MEK inhibitor PD0325901 significantly reduces the growth of papillary thyroid carcinoma cells in vitro and in vivo.
Molecular cancer therapeutics.
2010 Jul; 9(7):1968-76. doi:
10.1158/1535-7163.mct-10-0062
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Clinical cancer research : an official journal of the American Association for Cancer Research.
2010 Apr; 16(8):2450-7. doi:
10.1158/1078-0432.ccr-09-1920
. [PMID: 20332327] - Julius Leyton, Graham Smith, Yongjun Zhao, Meg Perumal, Quang-De Nguyen, Edward Robins, Erik Arstad, Eric O Aboagye. [18F]fluoromethyl-[1,2-2H4]-choline: a novel radiotracer for imaging choline metabolism in tumors by positron emission tomography.
Cancer research.
2009 Oct; 69(19):7721-8. doi:
10.1158/0008-5472.can-09-1419
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Nature.
2008 May; 453(7194):519-23. doi:
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. [PMID: 18497825] - Alan P Brown, Tage C G Carlson, Cho-Ming Loi, Michael J Graziano. Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration.
Cancer chemotherapy and pharmacology.
2007 Apr; 59(5):671-9. doi:
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