Dactolisib (BioDeep_00000858870)
代谢物信息卡片
Dactolisib
化学式: C30H23N5O (469.1903)
中文名称: Dactolisib
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)(C#N)C1=CC=C(C=C1)N2C3=C4C=C(C=CC4=NC=C3N(C2=O)C)C5=CC6=CC=CC=C6N=C5
InChI: InChI=1S/C30H23N5O/c1-30(2,18-31)22-9-11-23(12-10-22)35-28-24-15-19(21-14-20-6-4-5-7-25(20)32-16-21)8-13-26(24)33-17-27(28)34(3)29(35)36/h4-17H,1-3H3
描述信息
C274 - Antineoplastic Agent > C163758 - Targeted Therapy Agent > C2152 - Phosphatidylinositide 3-Kinase Inhibitor
C274 - Antineoplastic Agent > C2189 - Signal Transduction Inhibitor > C129824 - Antineoplastic Protein Inhibitor
COVID info from clinicaltrial, clinicaltrials, clinical trial, clinical trials
C471 - Enzyme Inhibitor > C129825 - Antineoplastic Enzyme Inhibitor
C274 - Antineoplastic Agent > C1742 - Angiogenesis Inhibitor
C471 - Enzyme Inhibitor > C1404 - Protein Kinase Inhibitor
D000970 - Antineoplastic Agents
Corona-virus
Coronavirus
SARS-CoV-2
COVID-19
SARS-CoV
COVID19
SARS2
SARS
同义名列表
2 个代谢物同义名
数据库引用编号
7 个数据库交叉引用编号
- ChEBI: CHEBI:71952
- KEGGdrug: D10552
- PubChem: 11977753
- DrugBank: DB11651
- ChEMBL: CHEMBL1879463
- CAS: 1028385-31-0
- CAS: 915019-65-7
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
- Xinglin Chen, Tongtong Zhang, Xiaohan Ren, Yuang Wei, Xu Zhang, Xinyue Zang, Xiran Ju, Chao Qin, Dongliang Xu. CHKB-AS1 enhances proliferation and resistance to NVP-BEZ235 of renal cancer cells via regulating the phosphorylation of MAP4 and PI3K/AKT/mTOR signaling.
European journal of medical research.
2023 Dec; 28(1):588. doi:
10.1186/s40001-023-01558-w. [PMID: 38093375] - Huarong Yang, Qing Li, Mingzhi Su, Fang Luo, Yahua Liu, Daoping Wang, Yanhua Fan. Design, synthesis, and biological evaluation of novel 6-(pyridin-3-yl) quinazolin-4(3H)-one derivatives as potential anticancer agents via PI3K inhibition.
Bioorganic & medicinal chemistry.
2021 09; 46(?):116346. doi:
10.1016/j.bmc.2021.116346. [PMID: 34403956] - Pratim Chowdhury, Dimuthu Perera, Reid T Powell, Tia Talley, Durga Nand Tripathi, Yong Sung Park, Michael A Mancini, Peter Davies, Clifford Stephan, Cristian Coarfa, Ruhee Dere. Therapeutically actionable signaling node to rescue AURKA driven loss of primary cilia in VHL-deficient cells.
Scientific reports.
2021 05; 11(1):10461. doi:
10.1038/s41598-021-89933-7. [PMID: 34002003] - Emily Golden, Rabab Rashwan, Eleanor A Woodward, Agustin Sgro, Edina Wang, Anabel Sorolla, Charlene Waryah, Wan Jun Tie, Elisabet Cuyàs, Magdalena Ratajska, Iwona Kardaś, Piotr Kozlowski, Elizabeth K M Johnstone, Heng B See, Ciara Duffy, Jeremy Parry, Kim A Lagerborg, Piotr Czapiewski, Javier A Menendez, Adam Gorczyński, Bartosz Wasag, Kevin D G Pfleger, Christina Curtis, Bum-Kyu Lee, Jonghwan Kim, Joseph Cursons, Nathan J Pavlos, Wojciech Biernat, Mohit Jain, Andrew J Woo, Andrew Redfern, Pilar Blancafort. The oncogene AAMDC links PI3K-AKT-mTOR signaling with metabolic reprograming in estrogen receptor-positive breast cancer.
Nature communications.
2021 03; 12(1):1920. doi:
10.1038/s41467-021-22101-7. [PMID: 33772001] - Fabian Lang, Lydia Wunderle, Susanne Badura, Eberhard Schleyer, Monika Brüggemann, Hubert Serve, Susanne Schnittger, Nicola Gökbuget, Heike Pfeifer, Sebastian Wagner, Kevin Ashelford, Gesine Bug, Oliver G Ottmann. A phase I study of a dual PI3-kinase/mTOR inhibitor BEZ235 in adult patients with relapsed or refractory acute leukemia.
BMC pharmacology & toxicology.
2020 09; 21(1):70. doi:
10.1186/s40360-020-00446-x. [PMID: 32993794] - Tian Xu, Tao Lin, Jingyuan Xie, Hong Ren, Nan Chen, Weiming Wang. Comparison of anti-peritoneal fibrotic effects between an mTORC1-specific blocker and a PI3K/mTOR dual-blocker.
Renal failure.
2019 Nov; 41(1):267-277. doi:
10.1080/0886022x.2019.1596818. [PMID: 30982374] - Haili Shi, Wouter N Leonhard, Niels J Sijbrandi, Mies J van Steenbergen, Marcel H A M Fens, Joep B van de Dikkenberg, Javier Sastre Toraño, Dorien J M Peters, Wim E Hennink, Robbert Jan Kok. Folate-dactolisib conjugates for targeting tubular cells in polycystic kidneys.
Journal of controlled release : official journal of the Controlled Release Society.
2019 01; 293(?):113-125. doi:
10.1016/j.jconrel.2018.11.019. [PMID: 30472374] - Cheng-Ming Hsu, Pai-Mei Lin, Hsin-Ching Lin, Yao-Te Tsai, Ming-Shao Tsai, Shau-Hsuan Li, Ching-Yuan Wu, Yao-Hsu Yang, Sheng-Fung Lin, Ming-Yu Yang. NVP-BEZ235 Attenuated Cell Proliferation and Migration in the Squamous Cell Carcinoma of Oral Cavities and p70S6K Inhibition Mimics its Effect.
International journal of molecular sciences.
2018 Nov; 19(11):. doi:
10.3390/ijms19113546. [PMID: 30423811] - Shima Gholizadeh, Jan A A M Kamps, Wim E Hennink, Robbert J Kok. PLGA-PEG nanoparticles for targeted delivery of the mTOR/PI3kinase inhibitor dactolisib to inflamed endothelium.
International journal of pharmaceutics.
2018 Sep; 548(2):747-758. doi:
10.1016/j.ijpharm.2017.10.032. [PMID: 29042337] - Jeremy S Logue, Alexander X Cartagena-Rivera, Richard S Chadwick. c-Src activity is differentially required by cancer cell motility modes.
Oncogene.
2018 04; 37(16):2104-2121. doi:
10.1038/s41388-017-0071-5. [PMID: 29379163] - Philip Earwaker, Caroline Anderson, Frances Willenbrock, Adrian L Harris, Andrew S Protheroe, Valentine M Macaulay. RAPTOR up-regulation contributes to resistance of renal cancer cells to PI3K-mTOR inhibition.
PloS one.
2018; 13(2):e0191890. doi:
10.1371/journal.pone.0191890. [PMID: 29389967] - Christophe Massard, Kim Nguyen Chi, Daniel Castellano, Johann de Bono, Gwenaelle Gravis, Luc Dirix, Jean-Pascal Machiels, Alain Mita, Begoña Mellado, Sabine Turri, Joan Maier, Denes Csonka, Arunava Chakravartty, Karim Fizazi. Phase Ib dose-finding study of abiraterone acetate plus buparlisib (BKM120) or dactolisib (BEZ235) in patients with castration-resistant prostate cancer.
European journal of cancer (Oxford, England : 1990).
2017 05; 76(?):36-44. doi:
10.1016/j.ejca.2017.01.024. [PMID: 28282611] - Nicole Willemsen-Seegers, Joost C M Uitdehaag, Martine B W Prinsen, Judith R F de Vetter, Jos de Man, Masaaki Sawa, Yusuke Kawase, Rogier C Buijsman, Guido J R Zaman. Compound Selectivity and Target Residence Time of Kinase Inhibitors Studied with Surface Plasmon Resonance.
Journal of molecular biology.
2017 02; 429(4):574-586. doi:
10.1016/j.jmb.2016.12.019. [PMID: 28043854] - Marco Falasca, Justin R Hamilton, Maria Selvadurai, Krithika Sundaram, Aleksandra Adamska, Philip E Thompson. Class II Phosphoinositide 3-Kinases as Novel Drug Targets.
Journal of medicinal chemistry.
2017 01; 60(1):47-65. doi:
10.1021/acs.jmedchem.6b00963. [PMID: 27644332] - Misu Lee, Ninelia Minaskan, Tobias Wiedemann, Martin Irmler, Johannes Beckers, Behrooz H Yousefi, Georgios Kaissis, Rickmer Braren, Iina Laitinen, Natalia S Pellegata. Targeting PI3K/mTOR signaling exerts potent antitumor activity in pheochromocytoma in vivo.
Endocrine-related cancer.
2017 01; 24(1):1-15. doi:
10.1530/erc-16-0324. [PMID: 27811202] - Klemens Hoegenauer, Nicolas Soldermann, Frédéric Stauffer, Pascal Furet, Nadege Graveleau, Alexander B Smith, Christina Hebach, Gregory J Hollingworth, Ian Lewis, Sascha Gutmann, Gabriele Rummel, Mark Knapp, Romain M Wolf, Joachim Blanz, Roland Feifel, Christoph Burkhart, Frédéric Zécri. Discovery and Pharmacological Characterization of Novel Quinazoline-Based PI3K Delta-Selective Inhibitors.
ACS medicinal chemistry letters.
2016 Aug; 7(8):762-7. doi:
10.1021/acsmedchemlett.6b00119. [PMID: 27563400] - Maria I Carlo, Ana M Molina, Yulia Lakhman, Sujata Patil, Kaitlin Woo, John DeLuca, Chung-Han Lee, James J Hsieh, Darren R Feldman, Robert J Motzer, Martin H Voss. A Phase Ib Study of BEZ235, a Dual Inhibitor of Phosphatidylinositol 3-Kinase (PI3K) and Mammalian Target of Rapamycin (mTOR), in Patients With Advanced Renal Cell Carcinoma.
The oncologist.
2016 07; 21(7):787-8. doi:
10.1634/theoncologist.2016-0145. [PMID: 27286790] - Zhen Ying Gan, Stephen Fitter, Kate Vandyke, Luen B To, Andrew C W Zannettino, Sally K Martin. The effect of the dual PI3K and mTOR inhibitor BEZ235 on tumour growth and osteolytic bone disease in multiple myeloma.
European journal of haematology.
2015 Apr; 94(4):343-54. doi:
10.1111/ejh.12436. [PMID: 25179233] - Silvina Grasso, Elena Tristante, Miguel Saceda, Pablo Carbonell, Leticia Mayor-López, Mar Carballo-Santana, Estefanía Carrasco-García, Lourdes Rocamora-Reverte, Pilar García-Morales, Fernando Carballo, José A Ferragut, Isabel Martínez-Lacaci. Resistance to Selumetinib (AZD6244) in colorectal cancer cell lines is mediated by p70S6K and RPS6 activation.
Neoplasia (New York, N.Y.).
2014 Oct; 16(10):845-60. doi:
10.1016/j.neo.2014.08.011. [PMID: 25379021] - João D Seixas, Sandra A Luengo-Arratta, Rosario Diaz, Manuel Saldivia, Domingo I Rojas-Barros, Pilar Manzano, Silvia Gonzalez, Manuela Berlanga, Terry K Smith, Miguel Navarro, Michael P Pollastri. Establishment of a structure-activity relationship of 1H-imidazo[4,5-c]quinoline-based kinase inhibitor NVP-BEZ235 as a lead for African sleeping sickness.
Journal of medicinal chemistry.
2014 Jun; 57(11):4834-48. doi:
10.1021/jm500361r. [PMID: 24805946] - Aifu Lin, Hai-Long Piao, Li Zhuang, Dos D Sarbassov, Li Ma, Boyi Gan. FoxO transcription factors promote AKT Ser473 phosphorylation and renal tumor growth in response to pharmacologic inhibition of the PI3K-AKT pathway.
Cancer research.
2014 Mar; 74(6):1682-93. doi:
10.1158/0008-5472.can-13-1729. [PMID: 24448243] - Hongyan Li, Xuefei Jin, Zhuo Zhang, Yuanyuan Xing, Xiangbo Kong. Inhibition of autophagy enhances apoptosis induced by the PI3K/AKT/mTor inhibitor NVP-BEZ235 in renal cell carcinoma cells.
Cell biochemistry and function.
2013 Jul; 31(5):427-33. doi:
10.1002/cbf.2917. [PMID: 23086777] - Maria Serova, Armand de Gramont, Annemilaï Tijeras-Raballand, Célia Dos Santos, Maria Eugenia Riveiro, Khemaies Slimane, Sandrine Faivre, Eric Raymond. Benchmarking effects of mTOR, PI3K, and dual PI3K/mTOR inhibitors in hepatocellular and renal cell carcinoma models developing resistance to sunitinib and sorafenib.
Cancer chemotherapy and pharmacology.
2013 May; 71(5):1297-307. doi:
10.1007/s00280-013-2129-6. [PMID: 23479136] - Hidenori Nishida, Eisei Sohara, Naohiro Nomura, Motoko Chiga, Dario R Alessi, Tatemitsu Rai, Sei Sasaki, Shinichi Uchida. Phosphatidylinositol 3-kinase/Akt signaling pathway activates the WNK-OSR1/SPAK-NCC phosphorylation cascade in hyperinsulinemic db/db mice.
Hypertension (Dallas, Tex. : 1979).
2012 Oct; 60(4):981-90. doi:
10.1161/hypertensionaha.112.201509. [PMID: 22949526] - Fan Lin, Gayathri Chandrasekaran, Mark C de Gooijer, Jos H Beijnen, Olaf van Tellingen. Determination of NVP-BEZ235, a dual PI3K and mTOR inhibitor, in human and mouse plasma and in mouse tissue homogenates by reversed-phase high-performance liquid chromatography with fluorescence detection.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.
2012 Jul; 901(?):9-17. doi:
10.1016/j.jchromb.2012.05.033. [PMID: 22727754] - Annett Mueller, Erika Bachmann, Monika Linnig, Katrin Khillimberger, Carl Christoph Schimanski, Peter R Galle, Markus Moehler. Selective PI3K inhibition by BKM120 and BEZ235 alone or in combination with chemotherapy in wild-type and mutated human gastrointestinal cancer cell lines.
Cancer chemotherapy and pharmacology.
2012 Jun; 69(6):1601-15. doi:
10.1007/s00280-012-1869-z. [PMID: 22543857] - 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] - Aymen A Elfiky, Saadia A Aziz, Patricia J Conrad, Summar Siddiqui, Wolfgang Hackl, Michel Maira, Camp L Robert, Harriet M Kluger. Characterization and targeting of phosphatidylinositol-3 kinase (PI3K) and mammalian target of rapamycin (mTOR) in renal cell cancer.
Journal of translational medicine.
2011 Aug; 9(?):133. doi:
10.1186/1479-5876-9-133. [PMID: 21834980] - Didier Roulin, Laurent Waselle, Anne Dormond-Meuwly, Marc Dufour, Nicolas Demartines, Olivier Dormond. Targeting renal cell carcinoma with NVP-BEZ235, a dual PI3K/mTOR inhibitor, in combination with sorafenib.
Molecular cancer.
2011 Jul; 10(?):90. doi:
10.1186/1476-4598-10-90. [PMID: 21791089] - Daniel C Cho, Matthew B Cohen, David J Panka, Michael Collins, Musie Ghebremichael, Michael B Atkins, Sabina Signoretti, James W Mier. The efficacy of the novel dual PI3-kinase/mTOR inhibitor NVP-BEZ235 compared with rapamycin in renal cell carcinoma.
Clinical cancer research : an official journal of the American Association for Cancer Research.
2010 Jul; 16(14):3628-38. doi:
10.1158/1078-0432.ccr-09-3022. [PMID: 20606035] - Kristen Pollizzi, Izabela Malinowska-Kolodziej, Michael Stumm, Heidi Lane, David Kwiatkowski. Equivalent benefit of mTORC1 blockade and combined PI3K-mTOR blockade in a mouse model of tuberous sclerosis.
Molecular cancer.
2009 Jun; 8(?):38. doi:
10.1186/1476-4598-8-38. [PMID: 19527517]
