General Information of Drug (ID: DMFGYKS)

Drug Name
MK-5108 Drug Info
Synonyms
1010085-13-8; VX-689; MK 5108; MK5108; MK-5108 (VX-689); UNII-H8J407531S; VX689; VX 689; CHEMBL3600873; H8J407531S; 4-(3-chloro-2-fluorophenoxy)-1-[[6-(1,3-thiazol-2-ylamino)pyridin-2-yl]methyl]cyclohexane-1-carboxylic acid; 4-(3-Chloranyl-2-Fluoranyl-Phenoxy)-1-[[6-(1,3-Thiazol-2-Ylamino)pyridin-2-Yl]methyl]cyclohexane-1-Carboxylic Acid; (1r,4r)-4-(3-chloro-2-fluorophenoxy)-1-((6-(thiazol-2-ylamino)pyridin-2-yl)methyl)cyclohexane-1-carboxylic acid; Cyclohexanecarboxylic acid,; MK-5108/VX-689
Indication
Disease Entry ICD 11 Status REF
Solid tumour/cancer 2A00-2F9Z Phase 1 [1]
Cross-matching ID
PubChem CID
24748204
ChEBI ID
CHEBI:125340
CAS Number
CAS 1010085-13-8
TTD Drug ID
DMFGYKS

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
Drug Status:
Clinical Trial Drug(s)
Drug(s) Targeting Aurora kinase B (AURKB)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT9283 DMQ94CT Solid tumour/cancer 2A00-2F9Z Phase 3 [3]
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [4]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [5]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [6]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
CYC116 DMUMHXT Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
AMG 900 DMASGXJ Solid tumour/cancer 2A00-2F9Z Phase 1 [9]
SNS-314 DMAC5F2 Solid tumour/cancer 2A00-2F9Z Phase 1 [10]
BI-847325 DMY4B6J Solid tumour/cancer 2A00-2F9Z Phase 1 [11]
R763 DME0CJ9 Haematological malignancy 2B33.Y Phase 1 [12]
⏷ Show the Full List of 10 Drug(s)
Drug(s) Targeting Aurora kinase A (AURKA)
Drug Name Drug ID Indication ICD 11 Highest Status REF
AT9283 DMQ94CT Solid tumour/cancer 2A00-2F9Z Phase 3 [3]
MLN8237 DMO8PT9 Solid tumour/cancer 2A00-2F9Z Phase 3 [13]
PHA-739358 DMGYBZI Prostate cancer 2C82.0 Phase 2 [4]
VX-680 DM93YKJ Solid tumour/cancer 2A00-2F9Z Phase 2 [5]
ABT-348 DMMZOYN Haematological malignancy 2B33.Y Phase 2 [6]
ENMD-2076 DMJZVPB Acute myeloid leukaemia 2A60 Phase 2 [4]
LY3295668 DM8RJTB Solid tumour/cancer 2A00-2F9Z Phase 1/2 [14]
HPP-607 DM5VSZR Solid tumour/cancer 2A00-2F9Z Phase 1 [7]
MLN8054 DMUANF3 Solid tumour/cancer 2A00-2F9Z Phase 1 [5]
CYC116 DMUMHXT Solid tumour/cancer 2A00-2F9Z Phase 1 [8]
⏷ 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
Aurora kinase A (AURKA) TTPS3C0 AURKA_HUMAN Inhibitor [2]
Aurora kinase B (AURKB) TT5LS6T AURKB_HUMAN Inhibitor [2]

References

1 ClinicalTrials.gov (NCT00543387) Treatment of Participants With Advanced and/or Refractory Solid Tumors (MK-5108-001 AM4). U.S. National Institutes of Health.
2 A novel c-Met inhibitor, MK8033, synergizes with carboplatin plus paclitaxel to inhibit ovarian cancer cell growth. Oncol Rep. 2013 May;29(5):2011-8.
3 A phase I trial of AT9283 (a selective inhibitor of aurora kinases) in children and adolescents with solid tumors: a Cancer Research UK study. Clin Cancer Res. 2015 Jan 15;21(2):267-73.
4 Cell cycle kinases as therapeutic targets for cancer. Nat Rev Drug Discov. 2009 Jul;8(7):547-66.
5 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
6 Preclinical characterization of ABT-348, a kinase inhibitor targeting the aurora, vascular endothelial growth factor receptor/platelet-derived growth factor receptor, and Src kinase families. J Pharmacol Exp Ther. 2012 Dec;343(3):617-27.
7 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: 1936).
8 Clinical pipeline report, company report or official report of Cyclacel.
9 Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. Cancer Res. 2010 Dec 1;70(23):9846-54.
10 SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo. Cancer Chemother Pharmacol. 2010 Mar;65(4):707-17.
11 doi: 10.1158/1535-7163.TARG-13-B281
12 Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen. J Cancer Res Clin Oncol. 2010 Jan;136(1):99-113.
13 Effect of Aurora A kinase inhibitor MLN8237 combined with rituximab on antitumor activity in preclinical B-cell non-Hodgkin's lymphoma models. Journal of Clinical Oncology, 2009:8553.
14 Aurora A-Selective Inhibitor LY3295668 Leads to Dominant Mitotic Arrest, Apoptosis in Cancer Cells, and Shows Potent Preclinical Antitumor Efficacy. Mol Cancer Ther. 2019 Dec;18(12):2207-2219.