Galunisertib (BioDeep_00000859050)
代谢物信息卡片
Galunisertib
化学式: C22H19N5O (369.159)
中文名称:
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC1=NC(=CC=C1)C2=NN3CCCC3=C2C4=C5C=C(C=CC5=NC=C4)C(=O)N
InChI: InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
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
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
同义名列表
1 个代谢物同义名
数据库引用编号
6 个数据库交叉引用编号
- ChEBI: CHEBI:137064
- KEGGdrug: D10437
- PubChem: 10090485
- DrugBank: DB11911
- ChEMBL: CHEMBL2364611
- CAS: 700874-72-2
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。
| 亚细胞结构定位 | 关联基因列表 |
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文献列表
- Lili Niu, Yao Liu, Nannan Li, Yang Wang, Lin Kang, Xiaomin Su, Ce Xu, Zanya Sun, Weicong Sang, Jingyuan Xu, Huishu Guo, Shun Shen. Oral probiotics microgel plus Galunisertib reduced TGF-β blockade resistance and enhanced anti-tumor immune responses in colorectal cancer.
International journal of pharmaceutics.
2024 Mar; 652(?):123810. doi:
10.1016/j.ijpharm.2024.123810. [PMID: 38244648] - Jonathan M Maher, Rui Zhang, Gopinath Palanisamy, Kimberly Perkins, Lynda Liu, Patrick Brassil, Alexander McNamara, Arthur Lo, Adam D Hughes, Jitendra Kanodia, Svitlana Kulyk, Kristen J Nikula, Hart S Dengler, Amy Scandurra, Ingrid Lua, Eric Harstad. Lung-restricted ALK5 inhibition avoids systemic toxicities associated with TGFβ pathway inhibition.
Toxicology and applied pharmacology.
2022 03; 438(?):115905. doi:
10.1016/j.taap.2022.115905. [PMID: 35122773] - James J Harding, Richard K Do, Amin Yaqubie, Ann Cleverly, Yumin Zhao, Ivelina Gueorguieva, Michael Lahn, Karim A Benhadji, Robin K Kelley, Ghassan K Abou-Alfa. Phase 1b study of galunisertib and ramucirumab in patients with advanced hepatocellular carcinoma.
Cancer medicine.
2021 05; 10(9):3059-3067. doi:
10.1002/cam4.3880. [PMID: 33811482] - Wenlong Li, Matthijs Tibben, Yaogeng Wang, Maria C Lebre, Hilde Rosing, Jos H Beijnen, Alfred H Schinkel. P-glycoprotein (MDR1/ABCB1) controls brain accumulation and intestinal disposition of the novel TGF-β signaling pathway inhibitor galunisertib.
International journal of cancer.
2020 03; 146(6):1631-1642. doi:
10.1002/ijc.32568. [PMID: 31304590] - Gianluigi Giannelli, Armando Santoro, Robin K Kelley, Ed Gane, Valerie Paradis, Ann Cleverly, Claire Smith, Shawn T Estrem, Michael Man, Shuaicheng Wang, Michael M Lahn, Eric Raymond, Karim A Benhadji, Sandrine Faivre. Biomarkers and overall survival in patients with advanced hepatocellular carcinoma treated with TGF-βRI inhibitor galunisertib.
PloS one.
2020; 15(3):e0222259. doi:
10.1371/journal.pone.0222259. [PMID: 32210440] - Emilia Bigaeva, Emilia Gore, Henricus A M Mutsaers, Dorenda Oosterhuis, Yong Ook Kim, Detlef Schuppan, Ruud A Bank, Miriam Boersema, Peter Olinga. Exploring organ-specific features of fibrogenesis using murine precision-cut tissue slices.
Biochimica et biophysica acta. Molecular basis of disease.
2020 01; 1866(1):165582. doi:
10.1016/j.bbadis.2019.165582. [PMID: 31676376] - M M Tibben, S Huijberts, W Li, A H Schinkel, A Gebretensae, H Rosing, J H Beijnen. Liquid chromatography-tandem mass spectrometric assay for the quantification of galunisertib in human plasma and the application in a pre-clinical study.
Journal of pharmaceutical and biomedical analysis.
2019 Sep; 173(?):169-175. doi:
10.1016/j.jpba.2019.05.037. [PMID: 31146172] - Davide Melisi, Rocio Garcia-Carbonero, Teresa Macarulla, Denis Pezet, Gael Deplanque, Martin Fuchs, Jorg Trojan, Mark Kozloff, Francesca Simionato, Ann Cleverly, Claire Smith, Shuaicheng Wang, Michael Man, Kyla E Driscoll, Shawn T Estrem, Michael M F Lahn, Karim A Benhadji, Josep Tabernero. TGFβ receptor inhibitor galunisertib is linked to inflammation- and remodeling-related proteins in patients with pancreatic cancer.
Cancer chemotherapy and pharmacology.
2019 05; 83(5):975-991. doi:
10.1007/s00280-019-03807-4. [PMID: 30887178] - Seddik Hammad, Elisabetta Cavalcanti, Julia Werle, Maria Lucia Caruso, Anne Dropmann, Antonia Ignazzi, Matthias Philip Ebert, Steven Dooley, Gianluigi Giannelli. Galunisertib modifies the liver fibrotic composition in the Abcb4Ko mouse model.
Archives of toxicology.
2018 07; 92(7):2297-2309. doi:
10.1007/s00204-018-2231-y. [PMID: 29808285] - Kenneth C Cassidy, Ivelina Gueorguieva, Colin Miles, Jessica Rehmel, Ping Yi, William J Ehlhardt. Disposition and metabolism of [14C]-galunisertib, a TGF-βRI kinase/ALK5 inhibitor, following oral administration in healthy subjects and mechanistic prediction of the effect of itraconazole on galunisertib pharmacokinetics.
Xenobiotica; the fate of foreign compounds in biological systems.
2018 Apr; 48(4):382-399. doi:
10.1080/00498254.2017.1323137. [PMID: 28436712] - Nemany Abdelhamid Nemany Hanafy, Alessandra Quarta, Marzia Maria Ferraro, Luciana Dini, Concetta Nobile, Maria Luisa De Giorgi, Sonia Carallo, Cinzia Citti, Antonio Gaballo, Giuseppe Cannazza, Rosaria Rinaldi, Gianluigi Giannelli, Stefano Leporatti. Polymeric Nano-Micelles as Novel Cargo-Carriers for LY2157299 Liver Cancer Cells Delivery.
International journal of molecular sciences.
2018 Mar; 19(3):. doi:
10.3390/ijms19030748. [PMID: 29509706] - Takayuki Kawai, Kentaro Yasuchika, Takamichi Ishii, Hokahiro Katayama, Elena Yukie Yoshitoshi, Satoshi Ogiso, Takahito Minami, Yuya Miyauchi, Hidenobu Kojima, Ryoya Yamaoka, Sadahiko Kita, Katsutaro Yasuda, Naoya Sasaki, Ken Fukumitsu, Etsuro Hatano, Shinji Uemoto. Identification of keratin 19-positive cancer stem cells associating human hepatocellular carcinoma using CYFRA 21-1.
Cancer medicine.
2017 Nov; 6(11):2531-2540. doi:
10.1002/cam4.1211. [PMID: 28965351] - David Capper, Andreas von Deimling, Alba A Brandes, Antoine F Carpentier, Santosh Kesari, Juan M Sepulveda-Sanchez, Helen R Wheeler, Olivier Chinot, Lawrence Cher, Joachim P Steinbach, Pol Specenier, Jordi Rodon, Ann Cleverly, Claire Smith, Ivelina Gueorguieva, Colin Miles, Susan C Guba, Durisala Desaiah, Shawn T Estrem, Michael M Lahn, Wolfgang Wick. Biomarker and Histopathology Evaluation of Patients with Recurrent Glioblastoma Treated with Galunisertib, Lomustine, or the Combination of Galunisertib and Lomustine.
International journal of molecular sciences.
2017 May; 18(5):. doi:
10.3390/ijms18050995. [PMID: 28481241] - Hung C Tran, Zesheng Wan, Michael A Sheard, Jianping Sun, Jeremy R Jackson, Jemily Malvar, Yibing Xu, Larry Wang, Richard Sposto, Eugene S Kim, Shahab Asgharzadeh, Robert C Seeger. TGFβR1 Blockade with Galunisertib (LY2157299) Enhances Anti-Neuroblastoma Activity of the Anti-GD2 Antibody Dinutuximab (ch14.18) with Natural Killer Cells.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2017 Feb; 23(3):804-813. doi:
10.1158/1078-0432.ccr-16-1743. [PMID: 27756784] - X Liu, M Yu, Y Chen, J Zhang. Galunisertib (LY2157299), a transforming growth factor-β receptor I kinase inhibitor, attenuates acute pancreatitis in rats.
Brazilian journal of medical and biological research = Revista brasileira de pesquisas medicas e biologicas.
2016 Aug; 49(9):e5388. doi:
10.1590/1414-431x20165388. [PMID: 27509307] - Yutaka Fujiwara, Hiroshi Nokihara, Yasuhide Yamada, Noboru Yamamoto, Kuniko Sunami, Hirofumi Utsumi, Hiroya Asou, Osamu TakahashI, Ken Ogasawara, Ivelina Gueorguieva, Tomohide Tamura. Phase 1 study of galunisertib, a TGF-beta receptor I kinase inhibitor, in Japanese patients with advanced solid tumors.
Cancer chemotherapy and pharmacology.
2015 Dec; 76(6):1143-52. doi:
10.1007/s00280-015-2895-4. [PMID: 26526984] - Richard J Kovacs, Giuliana Maldonado, Analia Azaro, Maria S Fernández, Federico L Romero, Juan M Sepulveda-Sánchez, Mary Corretti, Michael Carducci, Melda Dolan, Ivelina Gueorguieva, Ann L Cleverly, N Sokalingum Pillay, Jose Baselga, Michael M Lahn. Cardiac Safety of TGF-β Receptor I Kinase Inhibitor LY2157299 Monohydrate in Cancer Patients in a First-in-Human Dose Study.
Cardiovascular toxicology.
2015 Oct; 15(4):309-23. doi:
10.1007/s12012-014-9297-4. [PMID: 25488804] - Jordi Rodón, Michael Carducci, Juan M Sepulveda-Sánchez, Analía Azaro, Emiliano Calvo, Joan Seoane, Irene Braña, Elisabet Sicart, Ivelina Gueorguieva, Ann Cleverly, N Sokalingum Pillay, Durisala Desaiah, Shawn T Estrem, Luis Paz-Ares, Matthias Holdhoff, Jaishri Blakeley, Michael M Lahn, Jose Baselga. Pharmacokinetic, pharmacodynamic and biomarker evaluation of transforming growth factor-β receptor I kinase inhibitor, galunisertib, in phase 1 study in patients with advanced cancer.
Investigational new drugs.
2015 Apr; 33(2):357-70. doi:
10.1007/s10637-014-0192-4. [PMID: 25529192] - Jordi Rodon, Michael A Carducci, Juan M Sepulveda-Sánchez, Analia Azaro, Emiliano Calvo, Joan Seoane, Irene Braña, Elisabet Sicart, Ivelina Gueorguieva, Ann L Cleverly, N Sokalingum Pillay, Durisala Desaiah, Shawn T Estrem, Luis Paz-Ares, Matthias Holdhoff, Jaishri Blakeley, Michael M Lahn, Jose Baselga. First-in-human dose study of the novel transforming growth factor-β receptor I kinase inhibitor LY2157299 monohydrate in patients with advanced cancer and glioma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2015 Feb; 21(3):553-60. doi:
10.1158/1078-0432.ccr-14-1380. [PMID: 25424852] - Cheng Hua Jin, Maddeboina Krishnaiah, Domalapally Sreenu, Vura B Subrahmanyam, Kota S Rao, Hwa Jeong Lee, So-Jung Park, Hyun-Ju Park, Kiho Lee, Yhun Yhong Sheen, Dae-Kee Kim. Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/antifibrotic agent.
Journal of medicinal chemistry.
2014 May; 57(10):4213-38. doi:
10.1021/jm500115w. [PMID: 24786585] - Ivelina Gueorguieva, Ann L Cleverly, Anja Stauber, N Sada Pillay, Jordi A Rodon, Colin P Miles, Jonathan M Yingling, Michael M Lahn. Defining a therapeutic window for the novel TGF-β inhibitor LY2157299 monohydrate based on a pharmacokinetic/pharmacodynamic model.
British journal of clinical pharmacology.
2014 May; 77(5):796-807. doi:
10.1111/bcp.12256. [PMID: 24868575] - Shobha N Bhattachar, Everett J Perkins, Jeffrey S Tan, Lee J Burns. Effect of gastric pH on the pharmacokinetics of a BCS class II compound in dogs: utilization of an artificial stomach and duodenum dissolution model and GastroPlus,™ simulations to predict absorption.
Journal of pharmaceutical sciences.
2011 Nov; 100(11):4756-65. doi:
10.1002/jps.22669. [PMID: 21681753]
