Drug Information

Drug General Information
Drug ID
D03XAQ
Former ID
DIB015134
Drug Name
CH-5132799
Synonyms
CH-5033855; CH-5061565; CH-5089788; CH-5108135; CH-5111436; CH-5138134
Drug Type
Small molecular drug
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Phase 1 [531469], [542708]
Company
Chugai Pharmaceutical Co Ltd
Structure
Download
2D MOL

3D MOL
Formula
C15H19N7O3S
InChI
InChI=1S/C15H19N7O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21/h8-9H,2-7H2,1H3,(H2,16,17,18)
InChIKey
JEGHXKRHKHPBJD-UHFFFAOYSA-N
PubChem Compound ID
49784945
PubChem Substance ID
103057550, 124962287, 125088299, 136023437, 136348840, 136367527, 136920305, 136946642, 140632985, 141377281, 144115815, 162011954, 162038117, 162114957, 163620903, 163686224, 164041729, 174006491, 185997020, 223366076, 223389003, 223705062, 225372558, 228493084, 242060236, 246130933, 251965653, 252089855, 252215128, 252451780, 252471066, 252543417
Target and Pathway
Target(s) Phosphoinositide 3 kinase Target Info Inhibitor [531469]
PI3K beta Target Info Inhibitor [531469]
PI3K delta Target Info Inhibitor [531469]
PI3K alpha Target Info Inhibitor [531469]
BioCyc Pathway Superpathway of inositol phosphate compounds
3-phosphoinositide biosynthesisPWY-6371:Superpathway of inositol phosphate compounds
3-phosphoinositide biosynthesis
KEGG Pathway Inositol phosphate metabolism
ErbB signaling pathway
Ras signaling pathway
Rap1 signaling pathway
cGMP-PKG signaling pathway
cAMP signaling pathway
Chemokine signaling pathway
HIF-1 signaling pathway
FoxO signaling pathway
Phosphatidylinositol signaling system
Sphingolipid signaling pathway
mTOR signaling pathway
PI3K-Akt signaling pathway
AMPK 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
Insulin signaling pathway
Progesterone-mediated oocyte maturation
Estrogen signaling pathway
Prolactin signaling pathway
Thyroid hormone signaling pathway
Oxytocin signaling pathway
Regulation of lipolysis in adipocytes
Type II diabetes mellitus
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
Pathways in cancer
Viral carcinogenesis
Proteoglycans in cancer
MicroRNAs in cancer
Colorectal cancer
Renal cell carcinoma
Pancreatic cancer
Endometrial cancer
Glioma
Prostate cancer
Melanoma
Chronic myeloid leukemia
Acute myeloid leukemia
Small cell lung cancer
Non-small cell lung cancer
Central carbon metabolism in cancer
Choline metabolism in cancerhsa00562:Inositol phosphate metabolism
Choline metabolism in cancer
NetPath Pathway FSH Signaling Pathway
PANTHER Pathway Angiogenesis
Apoptosis signaling pathway
Axon guidance mediated by netrin
B cell activation
EGF receptor signaling pathway
Endothelin signaling pathway
FGF signaling pathway
Hypoxia response via HIF activation
Inflammation mediated by chemokine and cytokine signaling pathway
Insulin/IGF pathway-protein kinase B signaling cascade
Integrin signalling pathway
Interleukin signaling pathway
PDGF signaling pathway
PI3 kinase pathway
T cell activation
VEGF signaling pathway
p53 pathway
Ras Pathway
p53 pathway feedback loops 2
CCKR signaling map STP00005:Angiogenesis
p53 pathway feedback loops 2P00005:Angiogenesis
Pathway Interaction Database ErbB4 signaling events
LPA receptor mediated events
TRAIL signaling pathway
Signaling events mediated by TCPTP
FAS (CD95) signaling pathway
CXCR4-mediated signaling events
EGF receptor (ErbB1) signaling pathway
Class I PI3K signaling events
ErbB1 downstream signaling
ErbB2/ErbB3 signaling events
PDGFR-beta signaling pathway
Nephrin/Neph1 signaling in the kidney podocyte
Internalization of ErbB1
CXCR3-mediated signaling eventserbb4_pathway:ErbB4 signaling events
CXCR3-mediated signaling eventsfcer1pathway:Fc-epsilon receptor I signaling in mast cells
BCR signaling pathway
Insulin Pathway
GMCSF-mediated signaling events
Atypical NF-kappaB pathway
IL4-mediated signaling events
Plasma membrane estrogen receptor signaling
Signaling events mediated by Hepatocyte Growth Factor Receptor (c-Met)
Signaling events mediated by PTP1B
EPHB forward signaling
Osteopontin-mediated events
Reelin signaling pathway
Nectin adhesion pathway
CDC42 signaling events
Signaling events regulated by Ret tyrosine kinase
Angiopoietin receptor Tie2-mediated signaling
SHP2 signaling
Netrin-mediated signaling events
IL1-mediated signaling events
IL2-mediated signaling events
IGF1 pathway
IL5-mediated signaling events
IL2 signaling events mediated by PI3K
p75(NTR)-mediated signaling
E-cadherin signaling in the nascent adherens junction
Integrins in angiogenesis
IFN-gamma pathway
IL3-mediated signaling events
IL6-mediated signaling events
E-cadherin signaling in keratinocytes
Neurotrophic factor-mediated Trk receptor signaling
IL23-mediated signaling events
PDGFR-alpha signaling pathway
Signaling events mediated by the Hedgehog family
Nongenotropic Androgen signaling
CXCR3-mediated signaling events
VEGFR1 specific signals
Signaling events mediated by Stem cell factor receptor (c-Kit)
IL2 signaling events mediated by STAT5
Signaling events mediated by VEGFR1 and VEGFR2
PAR1-mediated thrombin signaling events
a6b1 and a6b4 Integrin signaling
Ephrin B reverse signaling
N-cadherin signaling events
Trk receptor signaling mediated by PI3K and PLC-gamma
EPHA2 forward signaling
VEGFR3 signaling in lymphatic endothelium
FGF signaling pathway
Signaling events mediated by focal adhesion kinase
PathWhiz Pathway 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 CellsPW000168:Phosphatidylinositol Phosphate MetabolismPW000143:Inositol Metabolism
Fc Epsilon Receptor I Signaling in Mast Cells
Reactome PI3K Cascade
GPVI-mediated activation cascade
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants
PI3K events in ERBB4 signaling
PIP3 activates AKT 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
CD28 dependent PI3K/Akt signaling
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 CBLR-HSA-109704:PI3K Cascade
Regulation of signaling by CBLR-HSA-114604:GPVI-mediated activation cascade
Regulation of signaling by CBL
Antigen activates B Cell Receptor (BCR) leading to generation of second messengersR-HSA-109704:PI3K Cascade
WikiPathways Toll-like receptor signaling pathway
Serotonin HTR1 Group and FOS Pathway
DNA Damage Response (only ATM dependent)
G13 Signaling Pathway
Regulation of Actin Cytoskeleton
Insulin Signaling
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
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)
Gastrin-CREB signalling pathway via PKC and MAPK
PIP3 activates AKT signaling
Integrated Pancreatic Cancer Pathway
Prostate Cancer
Signaling Pathways in Glioblastoma
TSLP Signaling Pathway
Regulation of Microtubule Cytoskeleton
TSH signaling pathway
SREBP signalling
TCR signaling
Signaling by PDGF
Signaling by Insulin receptor
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
Costimulation by the CD28 family
Cell surface interactions at the vascular wall
MicroRNAs in cardiomyocyte hypertrophy
Angiogenesis
Regulation of toll-like receptor signaling pathway
AMPK SignalingWP75:Toll-like receptor signaling pathway
Interferon type I signaling pathways
Focal Adhesion
IL-3 Signaling Pathway
Signaling by the B Cell Receptor (BCR)
Nanoparticle-mediated activation of receptor signaling
AMPK Signaling
References
Ref 531469The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.
Ref 542708(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: 7743).
Ref 531469The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81.

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