General Information of Drug (ID: DMEWQHP)

Drug Name
AZ-628 Drug Info
Synonyms Mutant B-Raf Kinase inhibitors, AstraZeneca; Mutant B-Raf (V600E) kinase inhibitors (cancer), AstraZeneca
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Investigative [1]
Cross-matching ID
PubChem CID
11676786
ChEBI ID
CHEBI:91354
CAS Number
CAS 878739-06-1
TTD Drug ID
DMEWQHP

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Clinical Trial Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Dabrafenib DMX6OE3 Melanoma 2C30 Approved [4]
Vemurafenib DM62UG5 Melanoma 2C30 Approved [5]
LGX818 DMNQXV8 Melanoma 2C30 Approved [6]
PLX8394 DMRTD7I Solid tumour/cancer 2A00-2F9Z Phase 2 [7]
CEP-32496 DMAO04B Solid tumour/cancer 2A00-2F9Z Phase 1/2 [8]
BGB-283 DMVYTG7 Solid tumour/cancer 2A00-2F9Z Phase 1/2 [9]
ARQ 736 DMP9ZT1 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
RO-5212054 DML4C3Q Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
ASN003 DMJCX6D Solid tumour/cancer 2A00-2F9Z Phase 1 [12]
BMS-908662 DM3K8VM Solid tumour/cancer 2A00-2F9Z Phase 1 [13]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [14]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [16]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [17]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [18]
Fulvestrant DM0YZC6 Breast cancer 2C60-2C65 Approved [19]
Secobarbital DM14RF5 Epilepsy 8A60-8A68 Approved [20]
Gefitinib DM15F0X Colon adenocarcinoma Approved [21]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [22]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [23]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ethanol DMDRQZU Chronic pain MG30 Approved [24]
Progesterone DMUY35B Amenorrhea GA20.0 Approved [15]
Carvedilol DMHTEAO Chronic heart failure BD1Z Approved [25]
Paclitaxel DMLB81S Breast carcinoma Approved [26]
Etoposide DMNH3PG Acute myelogenous leukaemia 2A41 Approved [27]
Cisplatin DMRHGI9 Adenocarcinoma 2D40 Approved [14]
Urokinase DM0GOUD Myocardial infarction BA41-BA43 Approved [28]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [29]
Sertraline DM0FB1J Coronary heart disease BA80.Z Approved [17]
Beta-carotene DM0RXBT Vitamin deficiency 5B55-5B71 Approved [18]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Affected By GTPase KRas (KRAS)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Simvastatin DM30SGU Arteriosclerosis BD40 Approved [30]
Quercetin DM3NC4M Obesity 5B81 Approved [31]
Isotretinoin DM4QTBN Acne vulgaris ED80 Approved [32]
Tiazofurin DM5JWV9 Solid tumour/cancer 2A00-2F9Z Approved [33]
Hydroquinone DM6AVR4 Melasma ED60.1 Approved [34]
Marinol DM70IK5 Anorexia nervosa cachexia 6B80 Approved [35]
Lovastatin DM9OZWQ Arteriosclerosis BD40 Approved [36]
Testosterone enanthate DMB6871 N. A. N. A. Approved [37]
Sevoflurane DMC9O43 Anaesthesia 9A78.6 Approved [38]
Valproate DMCFE9I Epilepsy 8A60-8A68 Approved [39]
⏷ 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
Serine/threonine-protein kinase B-raf (BRAF) TTWCGQT BRAF_HUMAN Inhibitor [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
GTPase KRas (KRAS) OT78QCN8 RASK_HUMAN Drug Response [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]

References

1 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. (Ligand id: 8475).
2 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. (Ligand id: 8475).
3 BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343. doi: 10.1371/journal.pone.0041343. Epub 2012 Jul 18.
4 Clinical pipeline report, company report or official report of GlaxoSmithKline (2011).
5 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
6 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
7 Identification of PLX4032-resistance mechanisms and implications for novel RAF inhibitors. Pigment Cell Melanoma Res. 2014 Mar;27(2):253-62.
8 Clinical pipeline report, company report or official report of Ambit Biosciences.
9 BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.
10 National Cancer Institute Drug Dictionary (drug id 688029).
11 National Cancer Institute Drug Dictionary (drug id 680347).
12 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
13 Clinical pipeline report, company report or official report of Exelixis (2011).
14 Treatment with anticancer agents induces dysregulation of specific Wnt signaling pathways in human ovarian luteinized granulosa cells in vitro. Toxicol Sci. 2013 Nov;136(1):183-92. doi: 10.1093/toxsci/kft175. Epub 2013 Aug 16.
15 Progesterone increases csk homologous kinase in HMC-1560 human mast cells and reduces cell proliferation. J Cell Biochem. 2007 Dec 1;102(5):1271-80. doi: 10.1002/jcb.21357.
16 Cannabidiol upregulates melanogenesis through CB1 dependent pathway by activating p38 MAPK and p42/44 MAPK. Chem Biol Interact. 2017 Aug 1;273:107-114. doi: 10.1016/j.cbi.2017.06.005. Epub 2017 Jun 7.
17 Sertraline, an antidepressant, induces apoptosis in hepatic cells through the mitogen-activated protein kinase pathway. Toxicol Sci. 2014 Feb;137(2):404-15. doi: 10.1093/toxsci/kft254. Epub 2013 Nov 5.
18 Growth stimulation of human pulmonary adenocarcinoma cells and small airway epithelial cells by beta-carotene via activation of cAMP, PKA, CREB and ERK1/2. Int J Cancer. 2006 Mar 15;118(6):1370-80. doi: 10.1002/ijc.21537.
19 Estrogen and pure antiestrogen fulvestrant (ICI 182 780) augment cell-matrigel adhesion of MCF-7 breast cancer cells through a novel G protein coupled estrogen receptor (GPR30)-to-calpain signaling axis. Toxicol Appl Pharmacol. 2014 Mar 1;275(2):176-81. doi: 10.1016/j.taap.2014.01.005. Epub 2014 Jan 17.
20 Inhibition of activator protein 1 by barbiturates is mediated by differential effects on mitogen-activated protein kinases and the small G proteins ras and rac-1. J Pharmacol Exp Ther. 2004 Dec;311(3):1232-40. doi: 10.1124/jpet.104.071332. Epub 2004 Jul 19.
21 Growth of hormone-dependent MCF-7 breast cancer cells is promoted by constitutive caveolin-1 whose expression is lost in an EGF-R-mediated manner during development of tamoxifen resistance. Breast Cancer Res Treat. 2010 Feb;119(3):575-91. doi: 10.1007/s10549-009-0355-8. Epub 2009 Mar 15.
22 Effect of histamine H1 receptor antagonists on TARC/CCL17 and MDC/CCL22 production from CD14+ cells induced by antigenic stimulation in vitro. Int Arch Allergy Immunol. 2011;155(1):38-51. doi: 10.1159/000318720. Epub 2010 Nov 25.
23 SIRT3 Mediates the Antioxidant Effect of Hydrogen Sulfide in Endothelial Cells. Antioxid Redox Signal. 2016 Feb 20;24(6):329-43. doi: 10.1089/ars.2015.6331. Epub 2015 Nov 10.
24 Downregulation of mitogen-activated protein kinases (MAPKs) in chronic ethanol-induced fatty liver. Toxicol Mech Methods. 2020 Jul;30(6):407-416. doi: 10.1080/15376516.2020.1747126. Epub 2020 Apr 1.
25 A unique mechanism of beta-blocker action: carvedilol stimulates beta-arrestin signaling. Proc Natl Acad Sci U S A. 2007 Oct 16;104(42):16657-62. doi: 10.1073/pnas.0707936104. Epub 2007 Oct 9.
26 The stent-eluting drugs sirolimus and paclitaxel suppress healing of the endothelium by induction of autophagy. Am J Pathol. 2009 Nov;175(5):2226-34.
27 Modulation of apoptosis in HaCaT keratinocytes via differential regulation of ERK signaling pathway by flavonoids. J Biol Chem. 2005 Sep 9;280(36):31498-507. doi: 10.1074/jbc.M505537200. Epub 2005 Jul 13.
28 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
29 Cannabidiol Modulates the Immunophenotype and Inhibits the Activation of the Inflammasome in Human Gingival Mesenchymal Stem Cells. Front Physiol. 2016 Nov 24;7:559. doi: 10.3389/fphys.2016.00559. eCollection 2016.
30 Cytotoxicity of simvastatin to pancreatic adenocarcinoma cells containing mutant ras gene. Jpn J Cancer Res. 1994 Jun;85(6):633-8. doi: 10.1111/j.1349-7006.1994.tb02406.x.
31 Quercetin and Its Fermented Extract as a Potential Inhibitor of Bisphenol A-Exposed HT-29 Colon Cancer Cells' Viability. Int J Mol Sci. 2023 Mar 15;24(6):5604. doi: 10.3390/ijms24065604.
32 Temporal changes in gene expression in the skin of patients treated with isotretinoin provide insight into its mechanism of action. Dermatoendocrinol. 2009 May;1(3):177-87.
33 Regulation of the signal transduction program by drugs. Adv Enzyme Regul. 1997;37:35-55. doi: 10.1016/s0065-2571(96)00025-8.
34 Hydroquinone-induced malignant transformation of TK6 cells by facilitating SIRT1-mediated p53 degradation and up-regulating KRAS. Toxicol Lett. 2016 Sep 30;259:133-142. doi: 10.1016/j.toxlet.2016.08.006. Epub 2016 Aug 8.
35 Delta9-tetrahydrocannabinol inhibits cytotrophoblast cell proliferation and modulates gene transcription. Mol Hum Reprod. 2006 May;12(5):321-33. doi: 10.1093/molehr/gal036. Epub 2006 Apr 5.
36 Combining prenylation inhibitors causes synergistic cytotoxicity, apoptosis and disruption of RAS-to-MAP kinase signalling in multiple myeloma cells. Br J Haematol. 2005 Sep;130(6):912-25. doi: 10.1111/j.1365-2141.2005.05696.x.
37 Transcriptional profiling of testosterone-regulated genes in the skeletal muscle of human immunodeficiency virus-infected men experiencing weight loss. J Clin Endocrinol Metab. 2007 Jul;92(7):2793-802. doi: 10.1210/jc.2006-2722. Epub 2007 Apr 17.
38 The differential cancer growth associated with anaesthetics in a cancer xenograft model of mice: mechanisms and implications of postoperative cancer recurrence. Cell Biol Toxicol. 2023 Aug;39(4):1561-1575. doi: 10.1007/s10565-022-09747-9. Epub 2022 Aug 12.
39 Stem cell transcriptome responses and corresponding biomarkers that indicate the transition from adaptive responses to cytotoxicity. Chem Res Toxicol. 2017 Apr 17;30(4):905-922.