General Information of Drug (ID: DMM7ZXR)

Drug Name
GSK2126458 Drug Info
Synonyms
1086062-66-9; Omipalisib; GSK-2126458; GSK 2126458; UNII-1X8F5A3NA0; 2,4-difluoro-N-(2-methoxy-5-(4-(pyridazin-4-yl)quinolin-6-yl)pyridin-3-yl)benzenesulfonamide; 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide; 2,4-Difluoro-N-[2-methoxy-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl]benzenesulfonamide; 1X8F5A3NA0; Omipalisib (GSK2126458, GSK458); C25H17F2N5O3S; Omipalisib [USAN:INN]
Indication
Disease Entry ICD 11 Status REF
Lymphoma 2A80-2A86 Phase 1 [1]
Cross-matching ID
PubChem CID
25167777
ChEBI ID
CHEBI:95093
CAS Number
CAS 1086062-66-9
TTD Drug ID
DMM7ZXR

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug(s) Targeting PI3-kinase gamma (PIK3CG)
Drug Name Drug ID Indication ICD 11 Highest Status REF
BAY 80-6946 DMLOS5R Follicular lymphoma 2A80 Approved [5]
IPI-145 DMWA24P Follicular lymphoma 2A80 Approved [6]
Buparlisib DM1WEHC Breast cancer 2C60-2C65 Phase 3 [7]
Enzastaurin DM5H0R9 Diffuse large B-cell lymphoma 2A81 Phase 3 [8]
Rigosertib DMOSTXF Myelodysplastic syndrome 2A37 Phase 3 [9]
GDC-0032 DMT4QHD Breast cancer 2C60-2C65 Phase 3 [8]
PQR309 DMMCYZ8 Squamous head and neck cell carcinom 2D60.0 Phase 2 [10]
SAR245409 DMQM7IL Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
XL147 DMML7BE Solid tumour/cancer 2A00-2F9Z Phase 2 [11]
SF1126 DML10K3 Head and neck cancer 2D42 Phase 2 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By Poly polymerase 1 (PARP1)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [13]
Gefitinib DM15F0X Colon adenocarcinoma Approved [14]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [15]
Nitric Oxide DM1RBYG Hypertension BA00-BA04 Approved [16]
Citalopram DM2G9AE Acute coronary syndrome BA41 Approved [17]
Ciprofloxacin XR DM2NLS9 Acute gonococcal cervicitis Approved [18]
Imipramine DM2NUH3 Depression 6A70-6A7Z Approved [17]
Colchicine DM2POTE Acute gout flare FA25.0 Approved [19]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [20]
Methotrexate DM2TEOL Anterior urethra cancer Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dexamethasone DMMWZET Acute adrenal insufficiency Approved [22]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [23]
Gefitinib DM15F0X Colon adenocarcinoma Approved [24]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [25]
Trametinib DM2JGQ3 Melanoma 2C30 Approved [3]
Quercetin DM3NC4M Obesity 5B81 Approved [26]
Romiplostim DM3U7SZ Thrombocytopenia 3B64 Approved [27]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [28]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [29]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [30]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [31]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [33]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [34]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [35]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [36]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [37]
Gefitinib DM15F0X Colon adenocarcinoma Approved [38]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [39]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [40]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [41]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [32]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [42]
Paclitaxel DMLB81S Breast carcinoma Approved [43]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [44]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [31]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [45]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [46]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [34]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [35]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [47]
Nicotine DMWX5CO Lung cancer 2C25.0 Approved [48]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [49]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [50]
Gefitinib DM15F0X Colon adenocarcinoma Approved [51]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [25]
Imiquimod DM1TMA3 Alopecia areata ED70.2 Approved [52]
Selenium DM25CGV N. A. N. A. Approved [53]
Methimazole DM25FL8 Hyperthyroidism 5A02 Approved [54]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [55]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [56]
Methotrexate DM2TEOL Anterior urethra cancer Approved [57]
Crizotinib DM4F29C Non-small-cell lung cancer 2C25.Y Approved [58]
Glucosamine DM4ZLFD Osteoarthritis FA00-FA05 Approved [29]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [59]
Aspirin DM672AH Acute coronary syndrome BA41 Approved [60]
Testosterone DM7HUNW Hot flushes GA30 Approved [61]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [62]
Capivasertib DM9SKW8 Breast cancer 2C60-2C65 Approved [47]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [63]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [64]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [55]
Thioridazine DM35M8J Schizophrenia 6A20 Approved [65]
Tretinoin DM49DUI Acne vulgaris ED80 Approved [66]
Arsenic trioxide DM61TA4 Acute lymphoblastic leukaemia 2A85 Approved [67]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [68]
Testosterone DM7HUNW Hot flushes GA30 Approved [61]
Imatinib DM7RJXL Acute lymphoblastic leukaemia 2A85 Approved [69]
Ciclosporin DMAZJFX Graft-versus-host disease 4B24 Approved [63]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [70]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
PI3-kinase gamma (PIK3CG) TTHBTOP PK3CG_HUMAN Modulator [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Eukaryotic translation initiation factor 4E-binding protein 1 (EIF4EBP1) OTHBQVD5 4EBP1_HUMAN Post-Translational Modifications [3]
Mitogen-activated protein kinase 1 (MAPK1) OTH85PI5 MK01_HUMAN Post-Translational Modifications [3]
Mitogen-activated protein kinase 3 (MAPK3) OTCYKGKO MK03_HUMAN Post-Translational Modifications [3]
Poly polymerase 1 (PARP1) OT310QSG PARP1_HUMAN Post-Translational Modifications [4]
RAC-alpha serine/threonine-protein kinase (AKT1) OT8H2YY7 AKT1_HUMAN Post-Translational Modifications [3]
Ribosomal protein S6 kinase beta-1 (RPS6KB1) OTAELNGX KS6B1_HUMAN Post-Translational Modifications [4]
Small ribosomal subunit protein eS6 (RPS6) OTT4D1LN RS6_HUMAN Post-Translational Modifications [4]

References

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2 Company report (GSK)
3 Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner. Clin Cancer Res. 2012 Aug 15;18(16):4345-55. doi: 10.1158/1078-0432.CCR-11-3227. Epub 2012 Jun 25.
4 Comparison of the effects of the PI3K/mTOR inhibitors NVP-BEZ235 and GSK2126458 on tamoxifen-resistant breast cancer cells. Cancer Biol Ther. 2011 Jun 1;11(11):938-46. doi: 10.4161/cbt.11.11.15527. Epub 2011 Jun 1.
5 BAY 80-6946 is a highly selective intravenous PI3K inhibitor with potent p110 and p110 activities in tumor cell lines and xenograft models.Mol Cancer Ther.2013 Nov;12(11):2319-30.
6 PI3K-delta and PI3K-gamma inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.
7 Targeting the phosphoinositide 3-kinase pathway in cancer. Nat Rev Drug Discov. 2009 Aug;8(8):627-44.
8 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
9 Phase I study of oral rigosertib (ON 01910.Na), a dual inhibitor of the PI3K and Plk1 pathways, in adult patients with advanced solid malignancies. Clin Cancer Res. 2014 Mar 15;20(6):1656-65.
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11 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2156).
12 An integrin-targeted, pan-isoform, phosphoinositide-3 kinase inhibitor, SF1126, has activity against multiple myeloma in vivo.Cancer Chemother Pharmacol.2013 Apr;71(4):867-81.
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19 Investigation of molecular mechanisms underlying the antiproliferative effects of colchicine against PC3 prostate cancer cells. Toxicol In Vitro. 2021 Jun;73:105138. doi: 10.1016/j.tiv.2021.105138. Epub 2021 Mar 6.
20 Sulindac enhances adenoviral vector expressing mda-7/IL-24-mediated apoptosis in human lung cancer. Mol Cancer Ther. 2005 Feb;4(2):291-304.
21 Methotrexate induces poly(ADP-ribose) polymerase-dependent, caspase 3-independent apoptosis in subsets of proliferating CD4+ T cells. Clin Exp Immunol. 2007 May;148(2):288-95. doi: 10.1111/j.1365-2249.2007.03335.x. Epub 2007 Feb 7.
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28 Differential modulation of PI3-kinase/Akt pathway during all-trans retinoic acid- and Am80-induced HL-60 cell differentiation revealed by DNA microarray analysis. Biochem Pharmacol. 2004 Dec 1;68(11):2177-86.
29 D-glucosamine down-regulates HIF-1alpha through inhibition of protein translation in DU145 prostate cancer cells. Biochem Biophys Res Commun. 2009 Apr 24;382(1):96-101. doi: 10.1016/j.bbrc.2009.02.129. Epub 2009 Feb 28.
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51 Dihydromyricetin suppresses tumor growth via downregulation of the EGFR/Akt/survivin signaling pathway. J Biochem Mol Toxicol. 2023 Jun;37(6):e23328. doi: 10.1002/jbt.23328. Epub 2023 Feb 19.
52 Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2015 Mar;35(3):1063-76. doi: 10.1111/liv.12626. Epub 2014 Jul 30.
53 Selenium and vitamin E: cell type- and intervention-specific tissue effects in prostate cancer. J Natl Cancer Inst. 2009 Mar 4;101(5):306-20.
54 Low-expressional IGF1 mediated methimazole-induced liver developmental toxicity in fetal mice. Toxicology. 2018 Sep 1;408:70-79. doi: 10.1016/j.tox.2018.07.004. Epub 2018 Jul 7.
55 Ribavirin augments doxorubicin's efficacy in human hepatocellular carcinoma through inhibiting doxorubicin-induced eIF4E activation. J Biochem Mol Toxicol. 2018 Jan;32(1). doi: 10.1002/jbt.22007. Epub 2017 Nov 7.
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57 Global molecular effects of tocilizumab therapy in rheumatoid arthritis synovium. Arthritis Rheumatol. 2014 Jan;66(1):15-23.
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59 Proteomics-based identification of differentially abundant proteins from human keratinocytes exposed to arsenic trioxide. J Proteomics Bioinform. 2014 Jul;7(7):166-178.
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64 Frenolicin B Targets Peroxiredoxin 1 and Glutaredoxin 3 to Trigger ROS/4E-BP1-Mediated Antitumor Effects. Cell Chem Biol. 2019 Mar 21;26(3):366-377.e12. doi: 10.1016/j.chembiol.2018.11.013. Epub 2019 Jan 17.
65 A gene signature-based approach identifies thioridazine as an inhibitor of phosphatidylinositol-3'-kinase (PI3K)/AKT pathway in ovarian cancer cells. Gynecol Oncol. 2011 Jan;120(1):121-7. doi: 10.1016/j.ygyno.2010.10.003. Epub 2010 Oct 29.
66 Benzodithiophenes potentiate differentiation of acute promyelocytic leukemia cells by lowering the threshold for ligand-mediated corepressor/coactivator exchange with retinoic acid receptor alpha and enhancing changes in all-trans-retinoic acid-regulated gene expression. Cancer Res. 2005 Sep 1;65(17):7856-65. doi: 10.1158/0008-5472.CAN-05-1056.
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68 Keratinocyte-derived IL-36gama plays a role in hydroquinone-induced chemical leukoderma through inhibition of melanogenesis in human epidermal melanocytes. Arch Toxicol. 2019 Aug;93(8):2307-2320.
69 A systems biology understanding of the synergistic effects of arsenic sulfide and Imatinib in BCR/ABL-associated leukemia. Proc Natl Acad Sci U S A. 2009 Mar 3;106(9):3378-83.
70 The neuroprotective action of the mood stabilizing drugs lithium chloride and sodium valproate is mediated through the up-regulation of the homeodomain protein Six1. Toxicol Appl Pharmacol. 2009 Feb 15;235(1):124-34.