PI-103

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H16N4O3
Molecular Weight	348.3553
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OC1=CC=CC(=C1)C2=NC(N3CCOCC3)=C4OC5=NC=CC=C5C4=N2

InChI

InChIKey=TUVCWJQQGGETHL-UHFFFAOYSA-N

InChI=1S/C19H16N4O3/c24-13-4-1-3-12(11-13)17-21-15-14-5-2-6-20-19(14)26-16(15)18(22-17)23-7-9-25-10-8-23/h1-6,11,24H,7-10H2

HIDE SMILES / InChI

Approval Year

Targets

Primary Target	Pharmacology	Potency
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 9 Target ID: P42336 Gene ID: 5290.0 Gene Symbol: PIK3CA Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.002 µM [IC50]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform 4 Target ID: P42338 Gene ID: 5291.0 Gene Symbol: PIK3CB Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.003 µM [IC50]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform 9 Target ID: O00329 Gene ID: 5293.0 Gene Symbol: PIK3CD Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.003 µM [IC50]
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform 5 Target ID: P48736 Gene ID: 5294.0 Gene Symbol: PIK3CG Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.015 µM [IC50]
Serine/threonine-protein kinase mTOR 35 Target ID: P42345 Gene ID: 2475.0 Gene Symbol: MTOR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.03 µM [IC50]
DNA-dependent protein kinase catalytic subunit 4 Target ID: P78527\|\|\|Q9UME3 Gene ID: 5591.0 Gene Symbol: PRKDC Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/19584227	Inhibitor 8297	0.023 µM [IC50]
PI3-kinase p110-alpha subunit 41 Target ID: CHEMBL4005 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27224913\| https://www.ncbi.nlm.nih.gov/pubmed/27658642	Inhibitor 8297
Serine/threonine-protein kinase mTOR 35 Target ID: CHEMBL2842 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27224913	Inhibitor 8297

PubMed

Title	Date	PubMed
The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of sorafenib-treated melanoma cells.	2010 Apr 1	19810100
PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways.	2010 Dec	21187475
GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways.	2011 Dec	21994956
Comprehensive analysis of kinase inhibitor selectivity.	2011 Oct 30	22037378
Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.	2011 Oct 30	22037377
PI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cells.	2012	23300809
A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.	2013 Apr 15	23398362

Name

Type

Language

PI-103

Common Name

English

PHENOL, 3-(4-(4-MORPHOLINYL)PYRIDO(3',2':4,5)FURO(3,2-D)PYRIMIDIN-2-YL)-

Systematic Name

English

PIK-103

Code

English

Code System Code Type Description

CAS

371935-74-9