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146535-11-7,MFCD00270913
Catalog No.:AA001E1G

146535-11-7 | Tyrphostin ag 1296

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1mg
99%
in stock  
$13.00   $9.00
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5mg
99%
in stock  
$32.00   $22.00
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10mg
99%
in stock  
$46.00   $32.00
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25mg
99%
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$77.00   $54.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA001E1G
Chemical Name:
Tyrphostin ag 1296
CAS Number:
146535-11-7
Molecular Formula:
C16H14N2O2
Molecular Weight:
266.2946
MDL Number:
MFCD00270913
SMILES:
COc1cc2nc(cnc2cc1OC)c1ccccc1
Properties
Properties
 
BP:
420.2°C at 760 mmHg  
Form:
Solid  
Stability:
Light Sensitive  
Storage:
Room Temperature;Light sensitive;Inert atmosphere;  

Computed Properties
 
Complexity:
307  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
20  
Hydrogen Bond Acceptor Count:
4  
Rotatable Bond Count:
3  
XLogP3:
2.8  

Literature

Title: Induction of HO-1 by carbon monoxide releasing molecule-2 attenuates thrombin-induced COX-2 expression and hypertrophy in primary human cardiomyocytes.

Journal: Toxicology and applied pharmacology 20151201

Title: A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery.

Journal: The Biochemical journal 20130415

Title: Fingolimod potentiates the effects of sunitinib malate in a rat breast cancer model.

Journal: Breast cancer research and treatment 20120701

Title: Small molecule screening identifies targetable zebrafish pigmentation pathways.

Journal: Pigment cell & melanoma research 20120301

Title: Uridine adenosine tetraphosphate (Up4A) is a strong inductor of smooth muscle cell migration via activation of the P2Y2 receptor and cross-communication to the PDGF receptor.

Journal: Biochemical and biophysical research communications 20120120

Title: HB-EGF and PDGF mediate reciprocal interactions of carcinoma cells with cancer-associated fibroblasts to support progression of uterine cervical cancers.

Journal: Cancer research 20111101

Title: Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity.

Journal: Nature biotechnology 20111101

Title: Combination of vascular endothelial growth factor receptor/platelet-derived growth factor receptor inhibition markedly improves the antiangiogenic efficacy for advanced stage mouse corneal neovascularization.

Journal: Graefe's archive for clinical and experimental ophthalmology = Albrecht von Graefes Archiv fur klinische und experimentelle Ophthalmologie 20111001

Title: PDGF-β receptor and PKC have no effect on angiotensin II-induced JAK2 and STAT1 phosphorylation in vascular smooth muscle cells under high glucose condition.

Journal: Journal of receptor and signal transduction research 20111001

Title: Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.

Journal: Bioorganic & medicinal chemistry letters 20101101

Title: Protein kinase C-delta transactivates platelet-derived growth factor receptor-alpha in mechanical strain-induced collagenase 3 (matrix metalloproteinase-13) expression by osteoblast-like cells.

Journal: The Journal of biological chemistry 20090918

Title: FGF2 is crucial for the development of bovine luteal endothelial networks in vitro.

Journal: Reproduction (Cambridge, England) 20090901

Title: VEGF/KDR loop is a target of AG1296 in acute myeloid leukaemia showing FLT3-internal tandem duplications.

Journal: British journal of haematology 20090601

Title: Bovine lactoferrin stimulates human corneal epithelial alkali wound healing in vitro.

Journal: Investigative ophthalmology & visual science 20090401

Title: Stem cell factor and interleukin-2/15 combine to enhance MAPK-mediated proliferation of human natural killer cells.

Journal: Blood 20090319

Title: BH3-only protein Bim more critical than Puma in tyrosine kinase inhibitor-induced apoptosis of human leukemic cells and transduced hematopoietic progenitors carrying oncogenic FLT3.

Journal: Blood 20090305

Title: Platelet-derived growth factor stimulates osteoprotegerin production in osteoblastic cells.

Journal: Journal of cellular physiology 20090201

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

Journal: Growth factors (Chur, Switzerland) 20090201

Title: Modulation of circadian rhythm of DNA synthesis in tumor cells by inhibiting platelet-derived growth factor signaling.

Journal: Journal of pharmacological sciences 20080801

Title: Inhibiting the platelet derived growth factor receptor increases signs of retinoic acid syndrome in myeloid differentiated HL-60 cells.

Journal: FEBS letters 20080723

Title: Resistance to FLT3 inhibition in an in vitro model of primary AML cells with a stem cell phenotype in a defined microenvironment.

Journal: Leukemia 20080701

Title: Gain-of-function mutations in the extracellular domain of KIT are common in canine mast cell tumors.

Journal: Molecular cancer research : MCR 20080701

Title: Angiotensin II activates extracellular signal-regulated kinase independently of receptor tyrosine kinases in renal smooth muscle cells: implications for blood pressure regulation.

Journal: The Journal of pharmacology and experimental therapeutics 20080101

Title: Potentiation by platelet-derived growth factor-BB of FGF-2-stimulated VEGF release in osteoblasts.

Journal: Journal of bone and mineral metabolism 20080101

Title: FLT3 regulates beta-catenin tyrosine phosphorylation, nuclear localization, and transcriptional activity in acute myeloid leukemia cells.

Journal: Leukemia 20071201

Title: Platelet-derived growth factor receptor regulates myeloid and monocytic differentiation of HL-60 cells.

Journal: Cancer research 20070815

Title: Hepatic stellate cell protrusions couple platelet-derived growth factor-BB to chemotaxis.

Journal: Hepatology (Baltimore, Md.) 20070601

Title: Platelet-derived growth factors and receptors in the rat corpus luteum: localization and identification of an effect on luteogenesis.

Journal: Biology of reproduction 20070301

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

Journal: Molecular vision 20070101

Title: Synergistic effect of arsenic trioxide and flt3 inhibition on cells with flt3 internal tandem duplication.

Journal: International journal of hematology 20061001

Title: Increase of C-type natriuretic peptide expression by serum and platelet-derived growth factor-BB in human aortic smooth muscle cells is dependent on protein kinase C activation.

Journal: Endocrinology 20060901

Title: P2Y12 receptor signalling towards PKB proceeds through IGF-I receptor cross-talk and requires activation of Src, Pyk2 and Rap1.

Journal: Cellular signalling 20060801

Title: Stimulatory autoantibodies to the PDGF receptor in systemic sclerosis.

Journal: The New England journal of medicine 20060622

Title: Fibroblast growth factor 2 and transforming growth factor beta1 synergism in human bronchial smooth muscle cell proliferation.

Journal: American journal of respiratory cell and molecular biology 20060601

Title: The role of PDGF receptor inhibitors and PI3-kinase signaling in the pathogenesis of corneal neovascularization.

Journal: Investigative ophthalmology & visual science 20060501

Title: Cell migration activated by platelet-derived growth factor receptor is blocked by an inverse agonist of the sphingosine 1-phosphate receptor-1.

Journal: FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20060301

Title: Tyrphostin-A47 inhibitable tyrosine phosphorylation of flagellar proteins is associated with distinct alteration of motility pattern in hamster spermatozoa.

Journal: Molecular reproduction and development 20060201

Title: The role of platelet-derived growth factor receptor in eotaxin signaling of eosinophils.

Journal: International archives of allergy and immunology 20060101

Title: Independent role of phosphoinositol-3-kinase (PI3K) and casein kinase II (CK-2) in EGFR and Her-2-mediated constitutive NF-kappaB activation in prostate cancer cells.

Journal: The Prostate 20051201

Title: The FLT3 internal tandem duplication mutation prevents apoptosis in interleukin-3-deprived BaF3 cells due to protein kinase A and ribosomal S6 kinase 1-mediated BAD phosphorylation at serine 112.

Journal: Cancer research 20050815

Title: Sphingosine-1-phosphate induces a PDGFR-dependent cell detachment via inhibiting beta1 integrin in HEK293 cells.

Journal: FEBS letters 20050718

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

Journal: Journal of medicinal chemistry 20050505

Title: Inhibitors of tyrosine kinase inhibit the production of urokinase plasminogen activator in human prostatic cancer cells.

Journal: APMIS : acta pathologica, microbiologica, et immunologica Scandinavica 20050501

Title: Platelet-derived growth factor-BB-induced human smooth muscle cell proliferation depends on basic FGF release and FGFR-1 activation.

Journal: Circulation research 20050204

Title: Specific locations of hydrophilic amino acids in constructed transmembrane ligands of the platelet-derived growth factor beta receptor.

Journal: Journal of molecular biology 20050128

Title: Enforced expression of an Flt3 internal tandem duplication in human CD34+ cells confers properties of self-renewal and enhanced erythropoiesis.

Journal: Blood 20050101

Title: Signal transduction of c-Kit receptor tyrosine kinase in CHRF myeloid leukemia cells.

Journal: Journal of cancer research and clinical oncology 20041201

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

Journal: Journal of medicinal chemistry 20041007

Title: Sphingosine 1-phosphate transactivates the platelet-derived growth factor beta receptor and epidermal growth factor receptor in vascular smooth muscle cells.

Journal: Circulation research 20040430

Title: Mutations in the tyrosine kinase domain of FLT3 define a new molecular mechanism of acquired drug resistance to PTK inhibitors in FLT3-ITD-transformed hematopoietic cells.

Journal: Blood 20040315

Title: Experimental systems for studying the role of G-protein-coupled receptors in receptor tyrosine kinase signal transduction.

Journal: Methods in enzymology 20040101

Title: Differential roles of WAVE1 and WAVE2 in dorsal and peripheral ruffle formation for fibroblast cell migration.

Journal: Developmental cell 20031001

Title: Signaling and distribution of NPR-Bi, the human splice form of the natriuretic peptide receptor type B.

Journal: American journal of physiology. Renal physiology 20030801

Title: Lysophosphatidic acid induces alpha1B-adrenergic receptor phosphorylation through G beta gamma, phosphoinositide 3-kinase, protein kinase C and epidermal growth factor receptor transactivation.

Journal: Biochimica et biophysica acta 20030721

Title: Sensitivity toward tyrosine kinase inhibitors varies between different activating mutations of the FLT3 receptor.

Journal: Blood 20030715

Title: Beta-platelet-derived growth factor receptor mediates motility and growth of Ewing's sarcoma cells.

Journal: Oncogene 20030417

Title: P2Y receptor-mediated stimulation of Müller glial cell DNA synthesis: dependence on EGF and PDGF receptor transactivation.

Journal: Investigative ophthalmology & visual science 20030301

Title: PDGF and FGF2 regulate oligodendrocyte progenitor responses to demyelination.

Journal: Journal of neurobiology 20030215

Title: Platelet-derived growth factor up-regulates the expression of transcription factors NF-E2, GATA-1 and c-Fos in megakaryocytic cell lines.

Journal: Cytokine 20030121

Title: Platelet-derived growth factor receptor kinase inhibitor AG1295 and inhibition of experimental proliferative vitreoretinopathy.

Journal: Japanese journal of ophthalmology 20030101

Title: Constitutive activation of c-kit by the juxtamembrane but not the catalytic domain mutations is inhibited selectively by tyrosine kinase inhibitors STI571 and AG1296.

Journal: International journal of hematology 20021201

Title: Ligand-independent trans-activation of the platelet-derived growth factor receptor by reactive oxygen species requires protein kinase C-delta and c-Src.

Journal: The Journal of biological chemistry 20021122

Title: Inhibition of aortic allograft vasculopathy by local delivery of platelet-derived growth factor receptor tyrosine-kinase blocker AG-1295.

Journal: Transplantation 20021115

Title: Lipoxin, leukotriene, and PDGF receptors cross-talk to regulate mesangial cell proliferation.

Journal: FASEB journal : official publication of the Federation of American Societies for Experimental Biology 20021101

Title: Study of the drug release mechanism from tyrphostin AG-1295-loaded nanospheres by in situ and external sink methods.

Journal: Journal of controlled release : official journal of the Controlled Release Society 20021030

Title: Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitor.

Journal: Leukemia 20021001

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

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

Title: Hypoxic induction of the hypoxia-inducible factor is mediated via the adaptor protein Shc in endothelial cells.

Journal: Circulation research 20020712

Title: Inhibition of platelet-derived growth factor actions in the embryonic testis influences normal cord development and morphology.

Journal: Biology of reproduction 20020301

Title: Formulation and delivery mode affect disposition and activity of tyrphostin-loaded nanoparticles in the rat carotid model.

Journal: Arteriosclerosis, thrombosis, and vascular biology 20010901

Title: A FLT3 tyrosine kinase inhibitor is selectively cytotoxic to acute myeloid leukemia blasts harboring FLT3 internal tandem duplication mutations.

Journal: Blood 20010801

Title: Tethering of the platelet-derived growth factor beta receptor to G-protein-coupled receptors. A novel platform for integrative signaling by these receptor classes in mammalian cells.

Journal: The Journal of biological chemistry 20010727

Title: Inhibition of FLT3-mediated transformation by use of a tyrosine kinase inhibitor.

Journal: Leukemia 20010701

Title: 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.

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

Title: Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation.

Journal: Cancer research 19941201

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