Idasanutlin (BioDeep_00000742821)
代谢物信息卡片
化学式: C31H29Cl2F2N3O4 (615.1503078)
中文名称: 伊达萨努特林(RG-7388)
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC(C)(C)CC1C(C(C(N1)C(=O)NC2=C(C=C(C=C2)C(=O)O)OC)C3=C(C(=CC=C3)Cl)F)(C#N)C4=C(C=C(C=C4)Cl)F
InChI: InChI=1S/C31H29Cl2F2N3O4/c1-30(2,3)14-24-31(15-36,19-10-9-17(32)13-21(19)34)25(18-6-5-7-20(33)26(18)35)27(38-24)28(39)37-22-11-8-16(29(40)41)12-23(22)42-4/h5-13,24-25,27,38H,14H2,1-4H3,(H,37,39)(H,40,41)/t24-,25-,27+,31-/m0/s1
描述信息
C274 - Antineoplastic Agent > C129839 - Apoptotic Pathway-targeting Antineoplastic Agent > C162996 - MDM2 Inhibitor
Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
同义名列表
2 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
- KEGGdrug: D11219
- PubChem: 53358942
- DrugBank: DB12325
- ChEMBL: CHEMBL2402737
- CAS: 1229705-06-9
- medchemexpress: HY-15676
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
- Kenichi Umehara, Yumi Cleary, Stephen Fowler, Neil Parrott, Dietrich Tuerck. Accelerating Clinical Development of Idasanutlin through a Physiologically Based Pharmacokinetic Modeling Risk Assessment for CYP450 Isoenzyme-Related Drug-Drug Interactions.
Drug metabolism and disposition: the biological fate of chemicals.
2022 03; 50(3):214-223. doi:
10.1124/dmd.121.000720. [PMID: 34937801] - Zhengyuan Zhou, Michael R Zalutsky, Satish K Chitneni. Fluorine-18 Labeling of the MDM2 Inhibitor RG7388 for PET Imaging: Chemistry and Preliminary Evaluation.
Molecular pharmaceutics.
2021 10; 18(10):3871-3881. doi:
10.1021/acs.molpharmaceut.1c00531. [PMID: 34523337] - Karen Yee, Cristina Papayannidis, Norbert Vey, Michael J Dickinson, Kevin R Kelly, Sarit Assouline, Margaret Kasner, Karen Seiter, Mark W Drummond, Sung-Soo Yoon, Je-Hwan Lee, Steven Blotner, Lori Jukofsky, William E Pierceall, Jianguo Zhi, Silke Simon, Brian Higgins, Gwen Nichols, Annabelle Monnet, Susanne Muehlbauer, Marion Ott, Lin-Chi Chen, Giovanni Martinelli. Murine double minute 2 inhibition alone or with cytarabine in acute myeloid leukemia: Results from an idasanutlin phase 1/1b study⋆.
Leukemia research.
2021 01; 100(?):106489. doi:
10.1016/j.leukres.2020.106489. [PMID: 33302031] - Albiruni R Abdul Razak, Wilson H Miller, Geoffrey L Uy, Steven Blotner, Anne-Marie Young, Brian Higgins, Lin-Chi Chen, Lia Gore. A phase 1 study of the MDM2 antagonist RO6839921, a pegylated prodrug of idasanutlin, in patients with advanced solid tumors.
Investigational new drugs.
2020 08; 38(4):1156-1165. doi:
10.1007/s10637-019-00869-2. [PMID: 31734832] - Zsuzsanna Pápai, Lin-Chi Chen, Daniel Da Costa, Steven Blotner, Faye Vazvaei, Michelle Gleave, Russell Jones, Jianguo Zhi. A single-center, open-label study investigating the excretion balance, pharmacokinetics, metabolism, and absolute bioavailability of a single oral dose of [14C]-labeled idasanutlin and an intravenous tracer dose of [13C]-labeled idasanutlin in a single cohort of patients with solid tumors.
Cancer chemotherapy and pharmacology.
2019 07; 84(1):93-103. doi:
10.1007/s00280-019-03851-0. [PMID: 31062077] - Lindi Chen, Fabio Pastorino, Philip Berry, Jennifer Bonner, Calum Kirk, Katrina M Wood, Huw D Thomas, Yan Zhao, Antonio Daga, Gareth J Veal, John Lunec, David R Newell, Mirco Ponzoni, Deborah A Tweddle. Preclinical evaluation of the first intravenous small molecule MDM2 antagonist alone and in combination with temozolomide in neuroblastoma.
International journal of cancer.
2019 06; 144(12):3146-3159. doi:
10.1002/ijc.32058. [PMID: 30536898] - Dongsheng Zhu, Haijun Guo, Yu Chang, Yun Ni, Lin Li, Zhi-Min Zhang, Piliang Hao, Yong Xu, Ke Ding, Zhengqiu Li. Cell- and Tissue-Based Proteome Profiling and Dual Imaging of Apoptosis Markers with Probes Derived from Venetoclax and Idasanutlin.
Angewandte Chemie (International ed. in English).
2018 07; 57(30):9284-9289. doi:
10.1002/anie.201802003. [PMID: 29768700] - Steven Blotner, Lin-Chi Chen, Cristiano Ferlini, Jianguo Zhi. Phase 1 summary of plasma concentration-QTc analysis for idasanutlin, an MDM2 antagonist, in patients with advanced solid tumors and AML.
Cancer chemotherapy and pharmacology.
2018 03; 81(3):597-607. doi:
10.1007/s00280-018-3534-7. [PMID: 29392451] - Kelli J Glenn, Li J Yu, Micaela B Reddy, Adrian J Fretland, Neil Parrott, Sazzad Hussain, Mary Palacios, Faye Vazvaei, Jianguo Zhi, Dietrich Tuerck. Investigating the effect of autoinduction in cynomolgus monkeys of a novel anticancer MDM2 antagonist, idasanutlin, and relevance to humans.
Xenobiotica; the fate of foreign compounds in biological systems.
2016 Aug; 46(8):667-76. doi:
10.3109/00498254.2015.1110761. [PMID: 26586447]