3-[6-(morpholin-4-yl)-8-oxa-3,5,10-triazatricyclo[7.4.0.0^{2,7}]trideca-1(9),2(7),3,5,10,12-hexaen-4-yl]phenol
| Title | Journal |
|---|---|
| PI-103 and Quercetin Attenuate PI3K-AKT Signaling Pathway in T- Cell Lymphoma Exposed to Hydrogen Peroxide. | PloS one 20160101 |
| Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. | The Biochemical journal 20130415 |
| Different PI 3-kinase inhibitors have distinct effects on endothelial permeability and leukocyte transmigration. | The international journal of biochemistry & cell biology 20121101 |
| PI3Kδ and PI3Kγ as targets for autoimmune and inflammatory diseases. | Journal of medicinal chemistry 20121025 |
| A yeast-based in vivo bioassay to screen for class I phosphatidylinositol 3-kinase specific inhibitors. | Journal of biomolecular screening 20120901 |
| Serum and glucocorticoid-regulated kinase 1 (SGK1) activation in breast cancer: requirement for mTORC1 activity associates with ER-alpha expression. | Breast cancer research and treatment 20120901 |
| Reconciling the different roles of Gsk3β in 'naïve' and 'primed' pluripotent stem cells. | Cell cycle (Georgetown, Tex.) 20120815 |
| PKI-587 and sorafenib targeting PI3K/AKT/mTOR and Ras/Raf/MAPK pathways synergistically inhibit HCC cell proliferation. | The Journal of surgical research 20120801 |
| Impact of oncogenic driver mutations on feedback between the PI3K and MEK pathways in cancer cells. | Bioscience reports 20120801 |
| Inhibition of the heat shock response by PI103 enhances the cytotoxicity of arsenic trioxide. | Toxicological sciences : an official journal of the Society of Toxicology 20120701 |
| The role of PI3K/mTOR inhibition in combination with sorafenib in hepatocellular carcinoma treatment. | Anticancer research 20120701 |
| A selective inhibitor reveals PI3Kγ dependence of T(H)17 cell differentiation. | Nature chemical biology 20120429 |
| Inhibition of chemokine (CXC motif) ligand 12/chemokine (CXC motif) receptor 4 axis (CXCL12/CXCR4)-mediated cell migration by targeting mammalian target of rapamycin (mTOR) pathway in human gastric carcinoma cells. | The Journal of biological chemistry 20120406 |
| Phosphoinositide 3-kinase/AKT/mTORC1/2 signaling determines sensitivity of Burkitt's lymphoma cells to BH3 mimetics. | Molecular cancer research : MCR 20120301 |
| Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo. | The Biochemical journal 20120215 |
| Preclinical activity of the novel orally bioavailable HSP90 inhibitor NVP-HSP990 against multiple myeloma cells. | Anticancer research 20120201 |
| Current development of the second generation of mTOR inhibitors as anticancer agents. | Chinese journal of cancer 20120101 |
| Inhibition of PI3K-Akt-mTOR signaling in glioblastoma by mTORC1/2 inhibitors. | Methods in molecular biology (Clifton, N.J.) 20120101 |
| Pharmacologic synergy between dual phosphoinositide-3-kinase and mammalian target of rapamycin inhibition and 5-fluorouracil in PIK3CA mutant gastric cancer cells. | Cancer biology & therapy 20120101 |
| Advances in establishment and analysis of three-dimensional tumor spheroid-based functional assays for target validation and drug evaluation. | BMC biology 20120101 |
| PI3K inhibition enhances doxorubicin-induced apoptosis in sarcoma cells. | PloS one 20120101 |
| Effects of small molecule inhibitors of PI3K/Akt/mTOR signaling on neuroblastoma growth in vitro and in vivo. | International journal of cancer 20111215 |
| GDC-0941 inhibits metastatic characteristics of thyroid carcinomas by targeting both the phosphoinositide-3 kinase (PI3K) and hypoxia-inducible factor-1α (HIF-1α) pathways. | The Journal of clinical endocrinology and metabolism 20111201 |
| Syntheses of phenylpyrazolodiazepin-7-ones as conformationally rigid analogs of aminopyrazole amide scaffold and their antiproliferative effects on cancer cells. | Bioorganic & medicinal chemistry 20111115 |
| Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. | Nature biotechnology 20111101 |
| Comprehensive analysis of kinase inhibitor selectivity. | Nature biotechnology 20111030 |
| Arsenic disulfide synergizes with the phosphoinositide 3-kinase inhibitor PI-103 to eradicate acute myeloid leukemia stem cells by inducing differentiation. | Carcinogenesis 20111001 |
| 5-Methoxyflavanone induces cell cycle arrest at the G2/M phase, apoptosis and autophagy in HCT116 human colon cancer cells. | Toxicology and applied pharmacology 20110801 |
| Differential regulation of CIDEA and CIDEC expression by insulin via Akt1/2- and JNK2-dependent pathways in human adipocytes. | Journal of lipid research 20110801 |
| Combination of PI3K/mTOR inhibitors: antitumor activity and molecular correlates. | Cancer research 20110701 |
| PDGF-induced vascular smooth muscle cell proliferation is associated with dysregulation of insulin receptor substrates. | American journal of physiology. Cell physiology 20110601 |
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. | European journal of medicinal chemistry 20110601 |
| Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies. | Neuro-oncology 20110601 |
| Secreted factors from brain endothelial cells maintain glioblastoma stem-like cell expansion through the mTOR pathway. | EMBO reports 20110501 |
| Transient PI3K inhibition induces apoptosis and overcomes HGF-mediated resistance to EGFR-TKIs in EGFR mutant lung cancer. | Clinical cancer research : an official journal of the American Association for Cancer Research 20110415 |
| Exploration of (S)-3-aminopyrrolidine as a potentially interesting scaffold for discovery of novel Abl and PI3K dual inhibitors. | European journal of medicinal chemistry 20110401 |
| Vertical inhibition of the mTORC1/mTORC2/PI3K pathway shows synergistic effects against melanoma in vitro and in vivo. | The Journal of investigative dermatology 20110201 |
| PI3K inhibitors prime neuroblastoma cells for chemotherapy by shifting the balance towards pro-apoptotic Bcl-2 proteins and enhanced mitochondrial apoptosis. | Oncogene 20110127 |
| Remodeling of VE-cadherin junctions by the human herpes virus 8 G-protein coupled receptor. | Oncogene 20110113 |
| A dual PI3K/mTOR inhibitor, PI-103, cooperates with stem cell-delivered TRAIL in experimental glioma models. | Cancer research 20110101 |
| Selective BRAFV600E inhibitor PLX4720, requires TRAIL assistance to overcome oncogenic PIK3CA resistance. | PloS one 20110101 |
| PI-103 and sorafenib inhibit hepatocellular carcinoma cell proliferation by blocking Ras/Raf/MAPK and PI3K/AKT/mTOR pathways. | Anticancer research 20101201 |
| Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | Chemistry & biology 20101124 |
| Akt and autophagy cooperate to promote survival of drug-resistant glioma. | Science signaling 20101109 |
| Effects of nominally selective inhibitors of the kinases PI3K, SGK1 and PKB on the insulin-dependent control of epithelial Na+ absorption. | British journal of pharmacology 20101001 |
| The phosphoinositide 3-kinase inhibitor PI-103 downregulates choline kinase alpha leading to phosphocholine and total choline decrease detected by magnetic resonance spectroscopy. | Cancer research 20100701 |
| Inducible EGFR T790M-mediated gefitinib resistance in non-small cell lung cancer cells does not modulate sensitivity to PI103 provoked autophagy. | Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20100601 |
| The dual PI3K/mTOR inhibitor PI-103 promotes immunosuppression, in vivo tumor growth and increases survival of sorafenib-treated melanoma cells. | International journal of cancer 20100401 |
| Shaping development of autophagy inhibitors with the structure of the lipid kinase Vps34. | Science (New York, N.Y.) 20100326 |
| Drugging the PI3 kinome: from chemical tools to drugs in the clinic. | Cancer research 20100315 |
| Chemogenomic profiling provides insights into the limited activity of irreversible EGFR Inhibitors in tumor cells expressing the T790M EGFR resistance mutation. | Cancer research 20100201 |
| Physical association of PDK1 with AKT1 is sufficient for pathway activation independent of membrane localization and phosphatidylinositol 3 kinase. | PloS one 20100101 |
| Chemical interrogation of FOXO3a nuclear translocation identifies potent and selective inhibitors of phosphoinositide 3-kinases. | The Journal of biological chemistry 20091009 |
| The pyridinylfuranopyrimidine inhibitor, PI-103, chemosensitizes glioblastoma cells for apoptosis by inhibiting DNA repair. | Oncogene 20091008 |
| A novel dual PI3Kalpha/mTOR inhibitor PI-103 with high antitumor activity in non-small cell lung cancer cells. | International journal of molecular medicine 20090701 |
| Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: from PI-103 through PI-540, PI-620 to the oral agent GDC-0941. | Molecular cancer therapeutics 20090701 |
| Inhibition of insulin-stimulated hydrogen peroxide production prevents stimulation of sodium transport in A6 cell monolayers. | American journal of physiology. Renal physiology 20090601 |
| Combination of PI3K/mTOR inhibition demonstrates efficacy in human chordoma. | Anticancer research 20090601 |
| Isoform-selective phosphoinositide 3'-kinase inhibitors inhibit CXCR4 signaling and overcome stromal cell-mediated drug resistance in chronic lymphocytic leukemia: a novel therapeutic approach. | Blood 20090528 |
| Relationship of deregulated signaling converging onto mTOR with prognosis and classification of lung adenocarcinoma shown by two independent in silico analyses. | Cancer research 20090501 |
| Dual targeting of AKT and mammalian target of rapamycin: a potential therapeutic approach for malignant peripheral nerve sheath tumor. | Molecular cancer therapeutics 20090501 |
| Dual inhibition of class IA phosphatidylinositol 3-kinase and mammalian target of rapamycin as a new therapeutic option for T-cell acute lymphoblastic leukemia. | Cancer research 20090415 |
| Inhibition of class I phosphoinositide 3-kinase activity impairs proliferation and triggers apoptosis in acute promyelocytic leukemia without affecting atra-induced differentiation. | Cancer research 20090201 |
| Molecular pharmacology of phosphatidylinositol 3-kinase inhibition in human glioma. | Cell cycle (Georgetown, Tex.) 20090201 |
| Effect of ZSTK474, a novel phosphatidylinositol 3-kinase inhibitor, on DNA-dependent protein kinase. | Biological & pharmaceutical bulletin 20090201 |
| High-throughput screening compatible cell-based assay for interrogating activated notch signaling. | Assay and drug development technologies 20090201 |
| Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases. | Nature chemical biology 20081101 |
| Dual inhibition of PI3Kalpha and mTOR as an alternative treatment for Kaposi's sarcoma. | Cancer research 20081015 |
| Genetic or pharmaceutical blockade of p110delta phosphoinositide 3-kinase enhances IgE production. | The Journal of allergy and clinical immunology 20081001 |
| The dual PI3 kinase/mTOR inhibitor PI-103 prevents p53 induction by Mdm2 inhibition but enhances p53-mediated mitochondrial apoptosis in p53 wild-type AML. | Leukemia 20080901 |
| PI-103, a dual inhibitor of Class IA phosphatidylinositide 3-kinase and mTOR, has antileukemic activity in AML. | Leukemia 20080901 |
| PDGF- and insulin/IGF-1-specific distinct modes of class IA PI 3-kinase activation in normal rat retinas and RGC-5 retinal ganglion cells. | Investigative ophthalmology & visual science 20080801 |
| Class I PI3 kinase inhibition by the pyridinylfuranopyrimidine inhibitor PI-103 enhances tumor radiosensitivity. | Cancer research 20080715 |
| Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma. | Molecular cancer therapeutics 20080401 |
| A quantitative analysis of kinase inhibitor selectivity. | Nature biotechnology 20080101 |
| A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases. | Proceedings of the National Academy of Sciences of the United States of America 20071218 |
| The selectivity of protein kinase inhibitors: a further update. | The Biochemical journal 20071215 |
| Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. | Bioorganic & medicinal chemistry 20070901 |
| A dual phosphoinositide-3-kinase alpha/mTOR inhibitor cooperates with blockade of epidermal growth factor receptor in PTEN-mutant glioma. | Cancer research 20070901 |
| Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors. | Bioorganic & medicinal chemistry letters 20070501 |
| A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. | Cell 20060519 |
| A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma. | Cancer cell 20060501 |