153436-54-5 | 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline

Packsize	Purity	Availability	Price	Discounted Price
50mg	96%	in stock	$32.00	$22.00
100mg	96%	in stock	$47.00	$33.00
250mg	96%	in stock	$82.00	$58.00
1g	96%	in stock	$144.00	$101.00
5g	96%	in stock	$455.00	$319.00

Description

• Catalog Number: AD70594
• Chemical Name: 4-(3-Bromoanilino)-6,7-dimethoxyquinazoline
• CAS Number: 153436-54-5
• Molecular Formula: C16H14BrN3O2
• Molecular Weight: 360.2053
• MDL Number: MFCD00934896
• SMILES: COc1cc2c(ncnc2cc1OC)Nc1cccc(c1)Br

Computed Properties

• Complexity: 360
• Covalently-Bonded Unit Count: 1
• Heavy Atom Count: 22
• Hydrogen Bond Acceptor Count: 5
• Hydrogen Bond Donor Count: 1
• Rotatable Bond Count: 4
• XLogP3: 4

Literature

• Regulation of ozone-induced lung inflammation by the epidermal growth factor receptor in mice.

  Environmental toxicology 20161201

• Role of EGF receptor ligands in TCDD-induced EGFR down-regulation and cellular proliferation.

  Chemico-biological interactions 20160625

• Function of DNA methyltransferase 3a in lead (Pb(2+) )-Induced Cyclooxygenase-2 gene.

  Environmental toxicology 20150901

• Nickel may contribute to EGFR mutation and synergistically promotes tumor invasion in EGFR-mutated lung cancer via nickel-induced microRNA-21 expression.

  Toxicology letters 20150819

• TG-interacting factor transcriptionally induced by AKT/FOXO3A is a negative regulator that antagonizes arsenic trioxide-induced cancer cell apoptosis.

  Toxicology and applied pharmacology 20150515

• Pb²⁺ induced IL-8 gene expression by extracellular signal-regulated kinases and the transcription factor, activator protein 1, in human gastric carcinoma cells.

  Environmental toxicology 20150301

• Pb2+ induces gastrin gene expression by extracellular signal-regulated kinases 1/2 and transcription factor activator protein 1 in human gastric carcinoma cells.

  Environmental toxicology 20150201

• Expression and regulation of stromal cell-derived factor-1 (SDF1) and chemokine CXC motif receptor 4 (CXCR4) in equine and bovine preovulatory follicles.

  Molecular and cellular endocrinology 20140625

• Areca nut components affect COX-2, cyclin B1/cdc25C and keratin expression, PGE2 production in keratinocyte is related to reactive oxygen species, CYP1A1, Src, EGFR and Ras signaling.

  PloS one 20140101

• Sodium arsenite exposure inhibits AKT and Stat3 activation, suppresses self-renewal and induces apoptotic death of embryonic stem cells.

  Apoptosis : an international journal on programmed cell death 20130201

• Activation of EGFR/MEK/ERK/AP-1 signaling mediated by 1,2-naphthoquinone, an atmospheric electrophile, in human pulmonary A549 cells.

  The Journal of toxicological sciences 20130101

• Discovery of 6-substituted 4-anilinoquinazolines with dioxygenated rings as novel EGFR tyrosine kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20120915

• A high-content biosensor-based screen identifies cell-permeable activators and inhibitors of EGFR function: implications in drug discovery.

  Journal of biomolecular screening 20120801

• Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.

  Bioorganic & medicinal chemistry 20120715

• Mechanism of β-catenin-mediated transcriptional regulation of epidermal growth factor receptor expression in glycogen synthase kinase 3 β-inactivated prostate cancer cells.

  The Journal of biological chemistry 20120525

• Tyrosine kinase inhibitors influence ABCG2 expression in EGFR-positive MDCK BCRP cells via the PI3K/Akt signaling pathway.

  ChemMedChem 20120401

• N⁴-(3-Bromophenyl)-7-(substituted benzyl) pyrrolo[2,3-d]pyrimidines as potent multiple receptor tyrosine kinase inhibitors: design, synthesis, and in vivo evaluation.

  Bioorganic & medicinal chemistry 20120401

• Inhibition of epidermal growth factor receptor tyrosine kinase ameliorates collagen-induced arthritis.

  Journal of immunology (Baltimore, Md. : 1950) 20120401

• N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.

  Bioorganic & medicinal chemistry 20120115

• Therapeutic and preventive effects of an epidermal growth factor receptor inhibitor on oral squamous cell carcinoma.

  The Journal of international medical research 20120101

• Stroma targeting nuclear imaging and radiopharmaceuticals.

  International journal of molecular imaging 20120101

• Molecular imaging with 11C-PD153035 PET/CT predicts survival in non-small cell lung cancer treated with EGFR-TKI: a pilot study.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20111001

• Suppression of TG-interacting factor sensitizes arsenic trioxide-induced apoptosis in human hepatocellular carcinoma cells.

  The Biochemical journal 20110901

• EGFR signaling suppresses osteoblast differentiation and inhibits expression of master osteoblastic transcription factors Runx2 and Osterix.

  Journal of cellular biochemistry 20110701

• Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20110401

• A novel hybrid peptide targeting EGFR-expressing cancers.

  European journal of cancer (Oxford, England : 1990) 20110301

• Evaluation of radioiodinated quinazoline derivative as a new ligand for EGF receptor tyrosine kinase activity using SPECT.

  Annals of nuclear medicine 20110201

• Involvement of the epidermal growth factor receptor in Pb²+-induced activation of cPLA₂/COX-2 genes and PGE₂ production in vascular smooth muscle cells.

  Toxicology 20110111

• Determining the binding mode and binding affinity constant of tyrosine kinase inhibitor PD153035 to DNA using optical tweezers.

  Biochemical and biophysical research communications 20110107

• Prediction of inhibitory activity of epidermal growth factor receptor inhibitors using grid search-projection pursuit regression method.

  PloS one 20110101

• Irreversible EGFR inhibitor EKB-569 targets low-LET γ-radiation-triggered rel orchestration and potentiates cell death in squamous cell carcinoma.

  PloS one 20110101

• Identification of the amyloid β-protein precursor and cystatin C as novel epidermal growth factor receptor regulated secretory proteins in nasopharyngeal carcinoma by proteomics.

  Journal of proteome research 20101203

• Design, synthesis, and DNA-binding of N-alkyl(anilino)quinazoline derivatives.

  Journal of medicinal chemistry 20101125

• Synthesis and in vitro study of pseudo-peptide thioureas containing α-aminophosphonate moiety as potential antitumor agents.

  European journal of medicinal chemistry 20101101

• Discovery of mitogen-activated protein kinase-interacting kinase 1 inhibitors by a comprehensive fragment-oriented virtual screening approach.

  Journal of medicinal chemistry 20100923

• Synthesis and initial tumor affinity testing of iodine-123 labelled EGFR-affine agents as potential imaging probes for hormone-refractory prostate cancer.

  European journal of medicinal chemistry 20100901

• Signaling through erbB receptors is a critical functional regulator in the mature cochlea.

  The European journal of neuroscience 20100901

• Epidermal growth factor receptor tyrosine kinase inhibitors induce CCL2 and CCL5 via reduction in IL-1R2 in keratinocytes.

  Experimental dermatology 20100801

• Gastrin-releasing peptide promotes the growth of HepG2 cells via EGFR-independent ERK1/2 activation.

  Oncology reports 20100801

• Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.

  Bioorganic & medicinal chemistry 20100715

• The contribution of a 2-amino group on receptor tyrosine kinase inhibition and antiangiogenic activity in 4-anilinosubstituted pyrrolo[2,3-d]pyrimidines.

  Bioorganic & medicinal chemistry letters 20100515

• Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.

  Bioorganic & medicinal chemistry 20100515

• F84, a quinazoline derivative, exhibits high potent antitumor activity against human gynecologic malignancies.

  Investigational new drugs 20100401

• Single agents with designed combination chemotherapy potential: synthesis and evaluation of substituted pyrimido[4,5-b]indoles as receptor tyrosine kinase and thymidylate synthase inhibitors and as antitumor agents.

  Journal of medicinal chemistry 20100225

• Exploring epidermal growth factor receptor (EGFR) inhibitor features: the role of fused dioxygenated rings on the quinazoline scaffold.

  Journal of medicinal chemistry 20100225

• B5, a novel pyrrole-substituted indolinone, exerts potent antitumor efficacy through G2/M cell cycle arrest.

  Investigational new drugs 20100201

• Diesel particle-induced transcriptional expression of p21 involves activation of EGFR, Src, and Stat3.

  American journal of respiratory cell and molecular biology 20100101

• Potent cardioprotective effect of the 4-anilinoquinazoline derivative PD153035: involvement of mitochondrial K(ATP) channel activation.

  PloS one 20100101

• EGFR tyrosine kinase inhibitor (PD153035) improves glucose tolerance and insulin action in high-fat diet-fed mice.

  Diabetes 20091201

• EFEMP1 binds the EGF receptor and activates MAPK and Akt pathways in pancreatic carcinoma cells.

  Biological chemistry 20091201

• NADPH oxidase and lipid raft-associated redox signaling are required for PCB153-induced upregulation of cell adhesion molecules in human brain endothelial cells.

  Toxicology and applied pharmacology 20091015

• Design, synthesis, and X-ray crystal structures of 2,4-diaminofuro[2,3-d]pyrimidines as multireceptor tyrosine kinase and dihydrofolate reductase inhibitors.

  Bioorganic & medicinal chemistry 20091015

• The unfolded protein response is activated in differentiating epidermal keratinocytes.

  The Journal of investigative dermatology 20090901

• Fluoride-induced cyclooxygenase-2 expression and prostaglandin E2 production in A549 human pulmonary epithelial cells.

  Toxicology letters 20090810

• Molecular imaging of EGFR: it's time to go beyond receptor expression.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20090701

• Lead acetate induces EGFR activation upstream of SFK and PKCalpha linkage to the Ras/Raf-1/ERK signaling.

  Toxicology and applied pharmacology 20090301

• Antitumor activity of a novel EGFR tyrosine kinase inhibitor against human lung carcinoma in vitro and in vivo.

  Investigational new drugs 20090201

• Growth factors involved in aqueous humour-induced lens cell proliferation.

  Growth factors (Chur, Switzerland) 20090201

• PET-based biodistribution and radiation dosimetry of epidermal growth factor receptor-selective tracer 11C-PD153035 in humans.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20090201

• Curcumin attenuates EGF-induced AQP3 up-regulation and cell migration in human ovarian cancer cells.

  Cancer chemotherapy and pharmacology 20081001

• Priming with EGFR tyrosine kinase inhibitor and EGF sensitizes ovarian cancer cells to respond to chemotherapeutical drugs.

  Cancer letters 20080808

• Identification of a potent, selective, and orally active leukotriene a4 hydrolase inhibitor with anti-inflammatory activity.

  Journal of medicinal chemistry 20080724

• HTS assays using a disease-relevant cell model for interrogating the MAP kinase pathway initiated by multiple receptors.

  Assay and drug development technologies 20080601

• Design, synthesis and biological evaluation of substituted pyrrolo[2,3-d]pyrimidines as multiple receptor tyrosine kinase inhibitors and antiangiogenic agents.

  Bioorganic & medicinal chemistry 20080515

• [Molecular imaging of epidermal growth factor receptor in glioma-bearing rats].

  Zhonghua zhong liu za zhi [Chinese journal of oncology] 20080501

• Towards predictive inhibitor design for the EGFR autophosphorylation activity.

  European journal of medicinal chemistry 20080401

• Activation of epidermal growth factor receptor by metal-ligand complexes decreases levels of extracellular amyloid beta peptide.

  The international journal of biochemistry & cell biology 20080101

• Biochemical assay-based selectivity profiling of clinically relevant kinase inhibitors on mutant forms of EGF receptor.

  Journal of receptor and signal transduction research 20080101

• Leptin stimulates the proliferation of human oesophageal adenocarcinoma cells via HB-EGF and Tgfalpha mediated transactivation of the epidermal growth factor receptor.

  British journal of biomedical science 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 DNA-binding epidermal growth factor-receptor inhibitor PD153035 and other DNA-intercalating cytotoxic drugs reactivate the expression of the retinoic acid receptor-beta tumor-suppressor gene in breast cancer cells.

  Differentiation; research in biological diversity 20071101

• Synthesis and bioactivities of 6,7,8-trimethoxy-N-aryl-4-aminoquinazoline derivatives.

  Bioorganic & medicinal chemistry 20071015

• Assessment of 11C-labeled-4-N-(3-bromoanilino)-6,7-dimethoxyquinazoline as a positron emission tomography agent to monitor epidermal growth factor receptor expression.

  Cancer science 20070901

• Signaling pathway for 2,3,7,8-tetrachlorodibenzo-p-dioxin-induced TNF-alpha production in differentiated THP-1 human macrophages.

  Experimental & molecular medicine 20070831

• Further characterization of the epidermal growth factor receptor ligand 11C-PD153035.

  Chinese medical journal 20070605

• Upregulation of retinoic acid receptor-beta by the epidermal growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB pathways.

  Journal of cellular physiology 20070601

• Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.

  Bioorganic & medicinal chemistry 20070601

• Protein C is an autocrine growth factor for human skin keratinocytes.

  The Journal of biological chemistry 20070504

• [Expressions of epidermal growth factor receptor signaling substances in gastric mucosal cells influenced by serum derived from rats treated with electroacupuncture at stomach meridian acupoints].

  Zhong xi yi jie he xue bao = Journal of Chinese integrative medicine 20070501

• Synthesis and bioactivity of 4-alkyl(aryl)thioquinazoline derivatives.

  Bioorganic & medicinal chemistry letters 20070415

• Blockage of epidermal growth factor receptor by quinazoline tyrosine kinase inhibitors suppresses growth of human hepatocellular carcinoma.

  Cancer letters 20070408

• EGF receptor clustering is induced by a 0.4 mT power frequency magnetic field and blocked by the EGF receptor tyrosine kinase inhibitor PD153035.

  Bioelectromagnetics 20070401

• Immortalization of human urothelial cells by human papillomavirus type 16 E6 and E7 genes in a defined serum-free system.

  Cell proliferation 20070401

• Diesel exhaust particulate-induced activation of Stat3 requires activities of EGFR and Src in airway epithelial cells.

  American journal of physiology. Lung cellular and molecular physiology 20070201

• Control of tight junctional sealing: role of epidermal growth factor.

  American journal of physiology. Renal physiology 20070201

• QSAR analysis of tyrosine kinase inhibitor using modified ant colony optimization and multiple linear regression.

  European journal of medicinal chemistry 20070101

• Epidermal growth factor receptor inhibition sensitizes renal cell carcinoma cells to the cytotoxic effects of bortezomib.

  Molecular cancer therapeutics 20070101

• Control of PDGF-induced reactive oxygen species (ROS) generation and signal transduction in human lens epithelial cells.

  Molecular vision 20070101

• Signal pathways involved in the regulation of prostaglandin E synthase-1 in human gingival fibroblasts.

  Cellular signalling 20061201

• EGFR-mediated expression of aquaporin-3 is involved in human skin fibroblast migration.

  The Biochemical journal 20061201

• Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.

  Journal of medicinal chemistry 20061116

• The tyrosine kinase inhibitor PD153035: implication of labeling position on radiometabolites formed in vitro.

  Nuclear medicine and biology 20061101

• UVB radiation induces expression of HIF-1alpha and VEGF through the EGFR/PI3K/DEC1 pathway.

  International journal of molecular medicine 20061001

• PPARgamma-regulated tight junction development during human urothelial cytodifferentiation.

  Journal of cellular physiology 20060801

• Inhibition of protein tyrosine phosphatase activity mediates epidermal growth factor receptor signaling in human airway epithelial cells exposed to Zn2+.

  Toxicology and applied pharmacology 20060701

• Inhibition of EGFR/PI3K/AKT cell survival pathway promotes TSA's effect on cell death and migration in human ovarian cancer cells.

  International journal of oncology 20060701

• Amphiregulin contributes to the transformed phenotype of human hepatocellular carcinoma cells.

  Cancer research 20060615

• The epidermal growth factor receptor (EGFR)-S442F mutant displays increased affinity for neuregulin-2beta and agonist-independent coupling with downstream signalling events.

  The Biochemical journal 20060515

• Indole-3-carbinol-induced death in cancer cells involves EGFR downregulation and is exacerbated in a 3D environment.

  Apoptosis : an international journal on programmed cell death 20060501

• COX-2-mediated stimulation of the lymphangiogenic factor VEGF-C in human breast cancer.

  British journal of cancer 20060424

• Transforming growth factor alpha attenuates the functional expression of AMPA receptors in cortical GABAergic neurons.

  Molecular and cellular neurosciences 20060401

• Opposite effect of ERK1/2 and JNK on p53-independent p21WAF1/CIP1 activation involved in the arsenic trioxide-induced human epidermoid carcinoma A431 cellular cytotoxicity.

  Journal of biomedical science 20060101

• Suppression of pro-metastasis phenotypes expression in malignant pleural mesothelioma by the PI3K inhibitor LY294002 or the MEK inhibitor UO126.

  Anticancer research 20060101

• Asbestos-induced activation of cell signaling pathways in human bronchial epithelial cells.

  Experimental lung research 20060101

• Epidermal growth factor-, transforming growth factor-beta-, retinoic acid- and 1,25-dihydroxyvitamin D3-regulated expression of the novel protein PTPIP51 in keratinocytes.

  Cells, tissues, organs 20060101

• Anilinodialkoxyquinazolines: screening epidermal growth factor receptor tyrosine kinase inhibitors for potential tumor imaging probes.

  Journal of medicinal chemistry 20051117

• p38 and EGF receptor kinase-mediated activation of the phosphatidylinositol 3-kinase/Akt pathway is required for Zn2+-induced cyclooxygenase-2 expression.

  American journal of physiology. Lung cellular and molecular physiology 20051101

• Targeted inhibition of transient activation of the EGFR-mediated cell survival pathway enhances paclitaxel-induced ovarian cancer cell death.

  International journal of oncology 20051101

• Transient activation of EGFR/AKT cell survival pathway and expression of survivin contribute to reduced sensitivity of human melanoma cells to betulinic acid.

  International journal of oncology 20050901

• Mechanism of thymus- and activation-regulated chemokine (TARC)/CCL17 production and its modulation by roxithromycin.

  The Journal of investigative dermatology 20050901

• Heparin-binding epidermal growth factor-like growth factor stimulates cell proliferation in cerebral cortical cultures through phosphatidylinositol 3'-kinase and mitogen-activated protein kinase.

  Journal of neuroscience research 20050815

• Up-regulation in endothelin-1 by Helicobacter pylori lipopolysaccharide interferes with gastric mucin synthesis via epidermal growth factor receptor transactivation.

  Scandinavian journal of gastroenterology 20050801

• Antagonistic regulation of swelling-activated Cl- current in rabbit ventricle by Src and EGFR protein tyrosine kinases.

  American journal of physiology. Heart and circulatory physiology 20050601

• Autocrine regulation of human urothelial cell proliferation and migration during regenerative responses in vitro.

  Experimental cell research 20050515

• Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 2. Identification of small-molecule inhibitors via coupling with virtual screening.

  Journal of medicinal chemistry 20050505

• The selective epidermal growth factor receptor tyrosine kinase inhibitor PD153035 suppresses expression of prometastasis phenotypes in malignant pleural mesothelioma cells in vitro.

  The Journal of thoracic and cardiovascular surgery 20050501

• Positive and negative transcriptional regulation of aromatase expression in human breast cancer tissue.

  The Journal of steroid biochemistry and molecular biology 20050501

• An EGF receptor inhibitor induces RAR-beta expression in breast and ovarian cancer cells.

  Biochemical and biophysical research communications 20050422

• Inhibition of the epidermal growth factor receptor increases expression of genes that stimulate inflammation, apoptosis, and cell attachment.

  Molecular cancer therapeutics 20050401

• High performance liquid chromatography analysis of a 4-anilinoquinazoline derivative (PD153035), a specific inhibitor of the epidermal growth factor receptor tyrosine kinase, in rat plasma.

  Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20050325

• Epidermal and hepatocyte growth factors, but not keratinocyte growth factor, modulate protein kinase Calpha translocation to the plasma membrane through 15(S)-hydroxyeicosatetraenoic acid synthesis.

  The Journal of biological chemistry 20050304

• Global kinase screening. Applications of frontal affinity chromatography coupled to mass spectrometry in drug discovery.

  Analytical chemistry 20050301

• Comparison of ELISA-based tyrosine kinase assays for screening EGFR inhibitors.

  Journal of receptor and signal transduction research 20050101

• Frontal affinity chromatography with MS detection of EphB2 tyrosine kinase receptor. 1. Comparison with conventional ELISA.

  Journal of medicinal chemistry 20041007

• [Role of PD153035 in the induction of apoptosis of XG-1 myeloma cell line].

  Zhongguo yi xue ke xue yuan xue bao. Acta Academiae Medicinae Sinicae 20041001

• Porphyromonas gingivalis lipopolysaccharide-induced up-regulation in endothelin-1 interferes with salivary mucin synthesis via epidermal growth factor receptor transactivation.

  IUBMB life 20041001

• Co-inhibition of epidermal growth factor receptor and type 1 insulin-like growth factor receptor synergistically sensitizes human malignant glioma cells to CD95L-induced apoptosis.

  Biochemical and biophysical research communications 20040827

• Involvement of MAP-kinase, PI3-kinase and EGF-receptor in the stimulatory effect of Neurotensin on DNA synthesis in PC3 cells.

  Regulatory peptides 20040815

• Salivary phospholipid secretion in response to beta-adrenergic stimulation is mediated by Src kinase-dependent epidermal growth factor receptor transactivation.

  Biochemical and biophysical research communications 20040521

• Prevention of renal vascular and glomerular fibrosis by epidermal growth factor receptor inhibition.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20040501

• Activation of peroxisome proliferator-activated receptor-gamma reverses squamous metaplasia and induces transitional differentiation in normal human urothelial cells.

  The American journal of pathology 20040501

• Role of PPARgamma and EGFR signalling in the urothelial terminal differentiation programme.

  Journal of cell science 20040415

• Heparin-binding epidermal growth factor cleavage mediates zinc-induced epidermal growth factor receptor phosphorylation.

  American journal of respiratory cell and molecular biology 20040401

• Regulation of parathyroid hormone-related protein gene expression by epidermal growth factor-family ligands in primary human keratinocytes.

  The Journal of endocrinology 20040401

• EphB4 signaling is capable of mediating ephrinB2-induced inhibition of cell migration.

  Biochemical and biophysical research communications 20040102

• Evaluation of novel epidermal growth factor receptor tyrosine kinase inhibitors.

  Breast cancer research and treatment 20040101

• Antiangiogenic and antitumor agents. Design, synthesis, and evaluation of novel 2-amino-4-(3-bromoanilino)-6-benzylsubstituted pyrrolo[2,3-d]pyrimidines as inhibitors of receptor tyrosine kinases.

  Bioorganic & medicinal chemistry 20031117

• Resistance to small molecule inhibitors of epidermal growth factor receptor in malignant gliomas.

  Cancer research 20031101

• Expression of ErbB receptors in ES cell-derived cardiomyocytes.

  Biochemical and biophysical research communications 20030912

• Mechanisms of Zn(2+)-induced signal initiation through the epidermal growth factor receptor.

  Toxicology and applied pharmacology 20030815

• Synergistic antiproliferative and apoptotic effects induced by epidermal growth factor receptor and protein kinase a inhibitors in human prostatic cancer cell lines.

  International journal of cancer 20030810

• Regulation of TGF-alpha-induced activation of AP-1 in the aging gastric mucosa.

  American journal of physiology. Gastrointestinal and liver physiology 20030801

• Epidermal growth factor inhibition of c-Myc-mediated apoptosis through Akt and Erk involves Bcl-xL upregulation in mammary epithelial cells.

  Experimental cell research 20030715

• Induction of aromatase (CYP19) expression in breast cancer cells through a nongenomic action of estrogen receptor alpha.

  Cancer research 20030701

• Mutation of threonine 766 in the epidermal growth factor receptor reveals a hotspot for resistance formation against selective tyrosine kinase inhibitors.

  The Journal of biological chemistry 20030425

• Quantitative image analysis of cellular protein translocation induced by magnetic microspheres: application to the EGF receptor.

  Cytometry. Part A : the journal of the International Society for Analytical Cytology 20030301

• Epidermal growth factor receptor trans-activation mediates the tonic and fibrogenic effects of endothelin in the aortic wall of transgenic mice.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20030201

• Synthesis and structure-activity relationships of 6,7-disubstituted 4-anilinoquinoline-3-carbonitriles. The design of an orally active, irreversible inhibitor of the tyrosine kinase activity of the epidermal growth factor receptor (EGFR) and the human epidermal growth factor receptor-2 (HER-2).

  Journal of medicinal chemistry 20030102

• PET screening of anticancer drugs. A faster route to drug/target evaluations in vivo.

  Methods in molecular medicine 20030101

• Enhanced antiangiogenic therapy of squamous cell carcinoma by combined endostatin and epidermal growth factor receptor-antisense therapy.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20021101

• Heparin-binding EGF-like growth factor gene transcription regulated by Cdx2 in the intestinal epithelium.

  American journal of physiology. Gastrointestinal and liver physiology 20021001

• Activation of proteinase-activated receptor 1 stimulates epithelial chloride secretion through a unique MAP kinase- and cyclo-oxygenase-dependent pathway.

  FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20021001

• 4-anilino-3-quinolinecarbonitriles: an emerging class of kinase inhibitors.

  Current topics in medicinal chemistry 20020901

• Regulation of Akt by EGF-R inhibitors, a possible mechanism of EGF-R inhibitor-enhanced TRAIL-induced apoptosis.

  Biochemical and biophysical research communications 20020712

• Okadaic acid-induced EGF receptor and MAP kinase activation does not require reactive oxygen species in primary keratinocytes.

  Archives of dermatological research 20020701

• EBV-expressing AGS gastric carcinoma cell sublines present increased motility and invasiveness.

  International journal of cancer 20020610

• Establishment and characterization of acquired resistance to the farnesyl protein transferase inhibitor R115777 in a human colon cancer cell line.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20020601

• Autocrine-mediated activation of STAT3 correlates with cell proliferation in breast carcinoma lines.

  The Journal of biological chemistry 20020517

• Role of Ras in metal-induced EGF receptor signaling and NF-kappaB activation in human airway epithelial cells.

  American journal of physiology. Lung cellular and molecular physiology 20020501

• Regulation of cultured rat hepatocyte proliferation by stellate cells.

  Journal of hepatology 20020501

• Prostaglandin E2 transactivates EGF receptor: a novel mechanism for promoting colon cancer growth and gastrointestinal hypertrophy.

  Nature medicine 20020301

• Activation of EGF receptors mediates pulmonary vasoconstriction induced by residual oil fly ash.

  Experimental lung research 20020101

• Transactivation of the epidermal growth factor receptor is involved in 12-O-tetradecanoylphorbol-13-acetate-induced signal transduction.

  The Journal of biological chemistry 20011214

• Lymnaea epidermal growth factor promotes axonal regeneration in CNS organ culture.

  The Journal of neuroscience : the official journal of the Society for Neuroscience 20011201

• Induction of EGFR-dependent and EGFR-independent signaling pathways by ultraviolet A irradiation.

  DNA and cell biology 20011201

• 1,4-dioxane-fused 4-anilinoquinazoline as inhibitors of epidermal growth factor receptor kinase.

  Archiv der Pharmazie 20011101

• Epidermal growth factor receptor signaling and the invasive phenotype of ovarian carcinoma cells.

  Journal of the National Cancer Institute 20010919

• Signaling-inactive epidermal growth factor receptor/ligand complexes in intact carcinoma cells by quinazoline tyrosine kinase inhibitors.

  Cancer research 20010801

• Differential utilization and localization of ErbB receptor tyrosine kinases in skin compared to normal and malignant keratinocytes.

  Neoplasia (New York, N.Y.) 20010701

• Epidermal growth factor induction of apolipoprotein A-I is mediated by the Ras-MAP kinase cascade and Sp1.

  The Journal of biological chemistry 20010427

• DNA interaction of the tyrosine protein kinase inhibitor PD153035 and its N-methyl analogue.

  Biochemistry 20010417

• Transmodulation of epidermal growth factor receptor mediates IL-1 beta-induced MMP-1 expression in cultured human keratinocytes.

  International journal of molecular medicine 20010301

• BIBX1382BS, but not AG1478 or PD153035, inhibits the ErbB kinases at different concentrations in intact cells.

  Biochemical and biophysical research communications 20010216

• Role of transforming growth factor-alpha in von Hippel--Lindau (VHL)(-/-) clear cell renal carcinoma cell proliferation: a possible mechanism coupling VHL tumor suppressor inactivation and tumorigenesis.

  Proceedings of the National Academy of Sciences of the United States of America 20010213

• A role for endogenous TGFalpha and associated signaling pathways in the differentiation of lens fiber cells.

  Journal of cellular physiology 20010201

• EGF receptor crosstalks with cytokine receptors leading to the activation of c-Jun kinase in response to UV irradiation in human keratinocytes.

  Cellular signalling 20010201

• New dermatological agents for the treatment of psoriasis.

  Journal of medicinal chemistry 20010201

• Allosteric inhibition of fructose-1,6-bisphosphatase by anilinoquinazolines.

  Bioorganic & medicinal chemistry letters 20010108

• Activation of the EGF receptor signaling pathway in human airway epithelial cells exposed to metals.

  The American journal of physiology 19991101

• Tyrosine kinase inhibitors. 9. Synthesis and evaluation of fused tricyclic quinazoline analogues as ATP site inhibitors of the tyrosine kinase activity of the epidermal growth factor receptor.

  Journal of medicinal chemistry 19960216

• Tyrosine kinase inhibitors. 8. An unusually steep structure-activity relationship for analogues of 4-(3-bromoanilino)-6,7-dimethoxyquinazoline (PD 153035), a potent inhibitor of the epidermal growth factor receptor.

  Journal of medicinal chemistry 19960105