Drug Information

Drug General Information
Drug ID
D0U3DP
Former ID
DIB015885
Drug Name
VS-5584
Drug Type
Small molecular drug
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Phase 1 [532167], [543098]
Company
Verastem
Structure
Download
2D MOL

3D MOL
Formula
C17H22N8O
InChI
InChI=1S/C17H22N8O/c1-10(2)25-11(3)21-14-13(12-8-19-16(18)20-9-12)22-17(23-15(14)25)24-4-6-26-7-5-24/h8-10H,4-7H2,1-3H3,(H2,18,19,20)
InChIKey
QYBGBLQCOOISAR-UHFFFAOYSA-N
PubChem Compound ID
46912230
PubChem Substance ID
99376660, 120919500, 163621035, 163686364, 169548936, 184824937, 208265527, 223382832, 223702838, 224593968, 226848955, 241383889, 245285867, 249683938, 250225766, 252074133, 252166594, 252216594, 252444830, 252473852
Target and Pathway
Target(s) Serine/threonine-protein kinase mTOR Target Info Modulator [532167]
Phosphoinositide 3 kinase Target Info Modulator [532167]
KEGG Pathway ErbB signaling pathway
HIF-1 signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK signaling pathway
Insulin signaling pathway
Thyroid hormone signaling pathway
Adipocytokine signaling pathway
Type II diabetes mellitus
Pathways in cancer
Proteoglycans in cancer
MicroRNAs in cancer
Glioma
Prostate cancer
Acute myeloid leukemia
Central carbon metabolism in cancer
Choline metabolism in cancerhsa00562:Inositol phosphate metabolism
Ras signaling pathway
Rap1 signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
FoxO signaling pathway
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
Apoptosis
Adrenergic signaling in cardiomyocytes
VEGF signaling pathway
Osteoclast differentiation
Focal adhesion
Signaling pathways regulating pluripotency of stem cells
Platelet activation
Toll-like receptor signaling pathway
Jak-STAT signaling pathway
Natural killer cell mediated cytotoxicity
T cell receptor signaling pathway
B cell receptor signaling pathway
Fc epsilon RI signaling pathway
Fc gamma R-mediated phagocytosis
TNF signaling pathway
Leukocyte transendothelial migration
Neurotrophin signaling pathway
Cholinergic synapse
Inflammatory mediator regulation of TRP channels
Regulation of actin cytoskeleton
Progesterone-mediated oocyte maturation
Estrogen signaling pathway
Prolactin signaling pathway
Oxytocin signaling pathway
Regulation of lipolysis in adipocytes
Non-alcoholic fatty liver disease (NAFLD)
Aldosterone-regulated sodium reabsorption
Carbohydrate digestion and absorption
Bacterial invasion of epithelial cells
Chagas disease (American trypanosomiasis)
Toxoplasmosis
Amoebiasis
Hepatitis C
Hepatitis B
Measles
Influenza A
HTLV-I infection
Epstein-Barr virus infection
Viral carcinogenesis
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Melanoma
Chronic myeloid leukemia
Small cell lung cancer
Non-small cell lung cancer
Choline metabolism in cancer
PANTHER Pathway Hypoxia response via HIF activation
Interleukin signaling pathway
Pathway Interaction Database IL4-mediated signaling events
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
IL12-mediated signaling events
CDC42 signaling events
LKB1 signaling events
Regulation of Telomerase
mTOR signaling pathway
CXCR4-mediated signaling events
EGFR-dependent Endothelin signaling events
IL2 signaling events mediated by PI3K
IFN-gamma pathway
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
CXCR3-mediated signaling events
Class I PI3K signaling events mediated by Akt
PathWhiz Pathway Leucine Stimulation on Insulin SignalingPW000143:Inositol Metabolism
Phosphatidylinositol Phosphate Metabolism
Intracellular Signalling Through Adenosine Receptor A2a and Adenosine
Intracellular Signalling Through Adenosine Receptor A2b and Adenosine
Fc Epsilon Receptor I Signaling in Mast Cells
Reactome PIP3 activates AKT signaling
Macroautophagy
mTORC1-mediated signalling
HSF1-dependent transactivation
CD28 dependent PI3K/Akt signaling
VEGFR2 mediated vascular permeability
TP53 Regulates Metabolic Genes
Constitutive Signaling by AKT1 E17K in CancerR-HSA-109704:PI3K Cascade
GPVI-mediated activation cascade
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
PI3K events in ERBB4 signaling
GAB1 signalosome
PI3K events in ERBB2 signaling
PI3K/AKT activation
Role of phospholipids in phagocytosis
Tie2 Signaling
Constitutive Signaling by Aberrant PI3K in Cancer
DAP12 signaling
Role of LAT2/NTAL/LAB on calcium mobilization
Nephrin interactions
Costimulation by the CD28 family
G beta:gamma signalling through PI3Kgamma
G alpha (q) signalling events
G alpha (12/13) signalling events
VEGFA-VEGFR2 Pathway
Interleukin-3, 5 and GM-CSF signaling
Constitutive Signaling by EGFRvIII
PI-3K cascade:FGFR1
PI-3K cascade:FGFR2
PI-3K cascade:FGFR3
PI-3K cascade:FGFR4
Interleukin receptor SHC signaling
Regulation of signaling by CBL
WikiPathways ErbB Signaling Pathway
Senescence and Autophagy in Cancer
Interferon type I signaling pathways
Insulin Signaling
EGF/EGFR Signaling Pathway
Wnt Signaling Pathway Netpath
Extracellular vesicle-mediated signaling in recipient cells
Cardiac Hypertrophic Response
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
PIP3 activates AKT signaling
Polycystic Kidney Disease Pathway
Alpha 6 Beta 4 signaling pathway
BDNF signaling pathway
Oncostatin M Signaling Pathway
Prostate Cancer
TSLP Signaling Pathway
FSH signaling pathway
Leptin signaling pathway
TSH signaling pathway
RANKL/RANK Signaling Pathway
SREBF and miR33 in cholesterol and lipid homeostasis
Integrated Breast Cancer Pathway
SREBP signalling
Signaling by Insulin receptor
Costimulation by the CD28 family
Type II diabetes mellitus
MicroRNAs in cardiomyocyte hypertrophy
TOR Signaling
AMPK SignalingWP75:Toll-like receptor signaling pathway
Serotonin HTR1 Group and FOS Pathway
DNA Damage Response (only ATM dependent)
G13 Signaling Pathway
Regulation of Actin Cytoskeleton
IL-4 Signaling Pathway
Copper homeostasis
Signaling of Hepatocyte Growth Factor Receptor
Transcriptional activation by NRF2
IL1 and megakaryotyces in obesity
Signaling by ERBB4
Signaling by ERBB2
Fc epsilon receptor (FCERI) signaling
PI Metabolism
Interleukin-2 signaling
Fcgamma receptor (FCGR) dependent phagocytosis
Signaling by SCF-KIT
DAP12 interactions
Gastrin-CREB signalling pathway via PKC and MAPK
Integrated Pancreatic Cancer Pathway
Signaling Pathways in Glioblastoma
Regulation of Microtubule Cytoskeleton
TCR signaling
Signaling by PDGF
Signaling by FGFR
Signaling by EGFR
NGF signalling via TRKA from the plasma membrane
Nephrin interactions
Interleukin-3, 5 and GM-CSF signaling
GPVI-mediated activation cascade
GPCR downstream signaling
Cell surface interactions at the vascular wall
Angiogenesis
Regulation of toll-like receptor signaling pathway
AMPK Signaling
References
Ref 532167VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61.
Ref 543098(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: 8382).
Ref 532167VS-5584, a novel and highly selective PI3K/mTOR kinase inhibitor for the treatment of cancer. Mol Cancer Ther. 2013 Feb;12(2):151-61.

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