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170364-57-5,MFCD11040980
Catalog No.:AA00ABH3

170364-57-5 | Enzastaurin

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Purity
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1mg
98%
in stock  
$11.00   $8.00
- +
5mg
98%
in stock  
$23.00   $16.00
- +
10mg
98%
in stock  
$34.00   $24.00
- +
50mg
98%
in stock  
$87.00   $61.00
- +
1g
98%
in stock  
$573.00   $401.00
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  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00ABH3
Chemical Name:
Enzastaurin
CAS Number:
170364-57-5
Molecular Formula:
C32H29N5O2
Molecular Weight:
515.6050
MDL Number:
MFCD11040980
SMILES:
O=C1NC(=O)C(=C1c1cn(c2c1cccc2)C1CCN(CC1)Cc1ccccn1)c1cn(c2c1cccc2)C
Properties
Computed Properties
 
Complexity:
974  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
39  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
5  
XLogP3:
3.7  

Downstream Synthesis Route
1-methyl-3-indoleacetimidicacidisopropylesterhydrochloride 
  1002115-95-8    170364-57-5 

[1]BioorganicandMedicinalChemistryLetters,2003,vol.13,p.1857-1859

[1]Tetrahedron,2003,vol.59,p.7215-7229

[2]Patent:WO2004/6928,2004,A1.Locationinpatent:Page/Pagecolumn13

[1]Tetrahedron,2003,vol.59,p.7215-7229

[2]BioorganicandMedicinalChemistryLetters,2011,vol.21,p.1649-1653

[1]Tetrahedron,2003,vol.59,p.7215-7229

[1]Tetrahedron,2003,vol.59,p.7215-7229

[2]Tetrahedron,2003,vol.59,p.7215-7229

[3]BioorganicandMedicinalChemistryLetters,2011,vol.21,p.1649-1653

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Title: NVP-BEZ235 alone and in combination in mantle cell lymphoma: an effective therapeutic strategy.

Journal: Expert opinion on investigational drugs 20121101

Title: Dose escalation and pharmacokinetics study of enzastaurin and sunitinib versus placebo and sunitinib in patients with metastatic renal cell carcinoma.

Journal: American journal of clinical oncology 20121001

Title: Combination of low doses of enzastaurin and lenalidomide has synergistic activity in B-non-Hodgkin lymphoma cell lines.

Journal: Annals of hematology 20121001

Title: A phase II study of enzastaurin in combination with erlotinib in patients with previously treated advanced non-small cell lung cancer.

Journal: Lung cancer (Amsterdam, Netherlands) 20121001

Title: A placebo-controlled, randomized phase II study of maintenance enzastaurin following whole brain radiation therapy in the treatment of brain metastases from lung cancer.

Journal: Lung cancer (Amsterdam, Netherlands) 20121001

Title: A multicenter phase II study of single-agent enzastaurin in previously treated Waldenstrom macroglobulinemia.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120915

Title: A double-blind, randomized, placebo-controlled, phase 2 study of maintenance enzastaurin with 5-fluorouracil/leucovorin plus bevacizumab after first-line therapy for metastatic colorectal cancer.

Journal: Cancer 20120901

Title: Protein phosphatase-2A activation is a critical step for enzastaurin activity in chronic lymphoid leukemia cells.

Journal: Leukemia & lymphoma 20120501

Title: Protein kinase C: a putative new target for the control of human medullary thyroid carcinoma cell proliferation in vitro.

Journal: Endocrinology 20120501

Title: Is there a world beyond bevacizumab in targeting angiogenesis in glioblastoma?

Journal: Expert opinion on investigational drugs 20120501

Title: Feasibility study of two schedules of sunitinib in combination with pemetrexed in patients with advanced solid tumors.

Journal: Investigational new drugs 20120401

Title: A phase I dose-escalation and pharmacokinetic study of enzastaurin and erlotinib in patients with advanced solid tumors.

Journal: Cancer chemotherapy and pharmacology 20120401

Title: A phase I study of LY317615 (enzastaurin) and temozolomide in patients with gliomas (EORTC trial 26054).

Journal: Neuro-oncology 20120301

Title: Enzastaurin has anti-tumour effects in lung cancers with overexpressed JAK pathway molecules.

Journal: British journal of cancer 20120227

Title: Novel targeted therapies for mantle cell lymphoma.

Journal: Oncotarget 20120201

Title: miR-122 regulates p53/Akt signalling and the chemotherapy-induced apoptosis in cutaneous T-cell lymphoma.

Journal: PloS one 20120101

Title: The protein kinase C inhibitor enzastaurin exhibits antitumor activity against uveal melanoma.

Journal: PloS one 20120101

Title: A phase II randomized study of cisplatin-pemetrexed plus either enzastaurin or placebo in chemonaive patients with advanced non-small cell lung cancer.

Journal: Oncology 20120101

Title: 14-3-3ζ interacts with stat3 and regulates its constitutive activation in multiple myeloma cells.

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Title: Novel therapies for aggressive B-cell lymphoma.

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Title: Pemetrexed plus platinum as the first-line treatment option for advanced non-small cell lung cancer: a meta-analysis of randomized controlled trials.

Journal: PloS one 20120101

Title: The first European interdisciplinary ewing sarcoma research summit.

Journal: Frontiers in oncology 20120101

Title: Oral enzastaurin in prostate cancer: a two-cohort phase II trial in patients with PSA progression in the non-metastatic castrate state and following docetaxel-based chemotherapy for castrate metastatic disease.

Journal: Investigational new drugs 20111201

Title: Effect of complementary pathway blockade on efficacy of combination enzastaurin and rapamycin.

Journal: Head & neck 20111201

Title: Phase II and pharmacogenomics study of enzastaurin plus temozolomide during and following radiation therapy in patients with newly diagnosed glioblastoma multiforme and gliosarcoma.

Journal: Neuro-oncology 20111201

Title: Preclinical emergence of vandetanib as a potent antitumour agent in mesothelioma: molecular mechanisms underlying its synergistic interaction with pemetrexed and carboplatin.

Journal: British journal of cancer 20111108

Title: Effects of heme oxygenase-1 on induction and development of chemically induced squamous cell carcinoma in mice.

Journal: Free radical biology & medicine 20111101

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Title: Impact of therapy on quality of life, neurocognitive function and their correlates in glioblastoma multiforme: a review.

Journal: Journal of neuro-oncology 20110901

Title: HDAC inhibitors potentiate the apoptotic effect of enzastaurin in lymphoma cells.

Journal: Apoptosis : an international journal on programmed cell death 20110901

Title: Antitumor activity of enzastaurin as radiation sensitizer in head and neck squamous cell carcinoma.

Journal: Head & neck 20110801

Title: Targeting protein kinase C by Enzastaurin restrains proliferation and secretion in human pancreatic endocrine tumors.

Journal: Endocrine-related cancer 20110801

Title: Enzastaurin hydrochloride for lymphoma: reassessing the results of clinical trials in light of recent advances in the biology of B-cell malignancies.

Journal: Expert opinion on investigational drugs 20110801

Title: Multicenter phase II trial of enzastaurin in patients with relapsed or refractory advanced cutaneous T-cell lymphoma.

Journal: Leukemia & lymphoma 20110801

Title: Rational combinations of enzastaurin with novel targeted agents for patients with B-cell non-Hodgkin's lymphoma.

Journal: Expert opinion on investigational drugs 20110801

Title: Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin.

Journal: The Journal of investigative dermatology 20110701

Title: A phase I safety study of enzastaurin plus bortezomib in the treatment of relapsed or refractory multiple myeloma.

Journal: American journal of hematology 20110701

Title: Targeting PKC-mediated signal transduction pathways using enzastaurin to promote apoptosis in acute myeloid leukemia-derived cell lines and blast cells.

Journal: Journal of cellular biochemistry 20110601

Title: A Gynecologic Oncology Group phase II trial of the protein kinase C-beta inhibitor, enzastaurin and evaluation of markers with potential predictive and prognostic value in persistent or recurrent epithelial ovarian and primary peritoneal malignancies.

Journal: Gynecologic oncology 20110601

Title: Pathway inhibition: emerging molecular targets for treating glioblastoma.

Journal: Neuro-oncology 20110601

Title: A new schedule of fotemustine in temozolomide-pretreated patients with relapsing glioblastoma.

Journal: Journal of neuro-oncology 20110501

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Journal: Journal of pharmaceutical and biomedical analysis 20110405

Title: Glycogen synthase kinase-3 (GSK-3) inhibition attenuates hepatocyte lipoapoptosis.

Journal: Journal of hepatology 20110401

Title: [11C]enzastaurin, the first design and radiosynthesis of a new potential PET agent for imaging of protein kinase C.

Journal: Bioorganic & medicinal chemistry letters 20110315

Title: APC +/- alters colonic fibroblast proteome in FAP.

Journal: Oncotarget 20110301

Title: Gemcitabine plus enzastaurin or single-agent gemcitabine in locally advanced or metastatic pancreatic cancer: results of a phase II, randomized, noncomparative study.

Journal: Investigational new drugs 20110201

Title: The need for third-line treatment in non-small cell lung cancer: an overview of new options.

Journal: Anticancer research 20110201

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Title: The anti-tumoral drug enzastaurin inhibits natural killer cell cytotoxicity via activation of glycogen synthase kinase-3β.

Journal: Biochemical pharmacology 20110115

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Journal: Evidence-based complementary and alternative medicine : eCAM 20110101

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Journal: Neuro-oncology 20110101

Title: Sunitinib malate synergistically potentiates anti-tumor effect of gemcitabine in human bladder cancer cells.

Journal: Korean journal of urology 20110101

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Journal: Journal of carcinogenesis 20110101

Title: Changes in gene expression and cellular architecture in an ovarian cancer progression model.

Journal: PloS one 20110101

Title: Gene Expression Differences between Enriched Normal and Chronic Myelogenous Leukemia Quiescent Stem/Progenitor Cells and Correlations with Biological Abnormalities.

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Journal: Radiation oncology (London, England) 20110101

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Journal: PloS one 20110101

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Journal: BMC cancer 20110101

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Journal: PloS one 20110101

Title: Targeted treatment for chronic lymphocytic leukemia.

Journal: OncoTargets and therapy 20110101

Title: Modulation of 4E-BP1 function as a critical determinant of enzastaurin-induced apoptosis.

Journal: Molecular cancer therapeutics 20101201

Title: [Chemotherapy and targeted treatments in glioblastomas].

Journal: Neuro-Chirurgie 20101201

Title: Randomized, phase II trial of pemetrexed and carboplatin with or without enzastaurin versus docetaxel and carboplatin as first-line treatment of patients with stage IIIB/IV non-small cell lung cancer.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20101201

Title: Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry.

Journal: Chemistry & biology 20101124

Title: Phase II, double-blind, randomized trial of capecitabine plus enzastaurin versus capecitabine plus placebo in patients with metastatic or recurrent breast cancer after prior anthracycline and taxane therapy.

Journal: Breast cancer research and treatment 20101101

Title: Maintenance and consolidation strategies in non-Hodgkin's lymphoma: A review of the data.

Journal: Current oncology reports 20101101

Title: Randomized, double-blinded, multicenter, phase II study of pemetrexed, carboplatin, and bevacizumab with enzastaurin or placebo in chemonaïve patients with stage IIIB/IV non-small cell lung cancer: Hoosier Oncology Group LUN06-116.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20101101

Title: Phase I dose escalation and pharmacokinetic study of oral enzastaurin (LY317615) in advanced solid tumors.

Journal: Cancer science 20101001

Title: Efficacy of the multi-kinase inhibitor enzastaurin is dependent on cellular signaling context.

Journal: Molecular cancer therapeutics 20101001

Title: Enzastaurin inhibits invasion and metastasis in lung cancer by diverse molecules.

Journal: British journal of cancer 20100907

Title: Enzastaurin (LY317615), a protein kinase C beta selective inhibitor, enhances antiangiogenic effect of radiation.

Journal: International journal of radiation oncology, biology, physics 20100801

Title: The impact of enzastaurin (LY317615.HCl) on CA125 biosynthesis and shedding in ovarian cancer cells.

Journal: Gynecologic oncology 20100701

Title: A phase I study of enzastaurin combined with pemetrexed in advanced non-small cell lung cancer.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20100701

Title: Enzastaurin plus temozolomide with radiation therapy in glioblastoma multiforme: a phase I study.

Journal: Neuro-oncology 20100601

Title: A window of opportunity phase II study of enzastaurin in chemonaive patients with asymptomatic metastatic colorectal cancer.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20100501

Title: Long-term follow-up of chemonaive patients with asymptomatic metastatic colorectal cancer treated with enzastaurin in a window of opportunity phase II study.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20100501

Title: Prognostic impact of protein kinase C beta II expression in R-CHOP-treated diffuse large B-cell lymphoma patients.

Journal: Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc 20100501

Title: Epithelial-to-mesenchymal transition and oncogenic Ras expression in resistance to the protein kinase Cbeta inhibitor enzastaurin in colon cancer cells.

Journal: Molecular cancer therapeutics 20100501

Title: Protein kinase C-beta gene variants, pathway activation, and enzastaurin activity in lung cancer.

Journal: Clinical lung cancer 20100501

Title: Effects of enzastaurin, alone or in combination, on signaling pathway controlling growth and survival of B-cell lymphoma cell lines.

Journal: Leukemia & lymphoma 20100401

Title: Phase II, double-blinded, randomized study of enzastaurin plus pemetrexed as second-line therapy in patients with advanced non-small cell lung cancer.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20100301

Title: Enzastaurin in the treatment of recurrent glioblastoma: a promise that did not materialize.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20100301

Title: Phase III study of enzastaurin compared with lomustine in the treatment of recurrent intracranial glioblastoma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20100301

Title: Combined RNA-expression and 2D-PAGE-screening identifies comprehensive interaction networks affected after bortezomib or enzastaurin exposure of mantle cell lymphoma.

Journal: Talanta 20100215

Title: A phase I/II trial of enzastaurin in patients with recurrent high-grade gliomas.

Journal: Neuro-oncology 20100201

Title: Protein kinase Cbeta modulates ligand-induced cell surface death receptor accumulation: a mechanistic basis for enzastaurin-death ligand synergy.

Journal: The Journal of biological chemistry 20100108

Title: Pharmacological aspects of the enzastaurin-pemetrexed combination in non-small cell lung cancer (NSCLC).

Journal: Current drug targets 20100101

Title: Recruitment of PKC-betaII to lipid rafts mediates apoptosis-resistance in chronic lymphocytic leukemia expressing ZAP-70.

Journal: Leukemia 20100101

Title: Synergistic antifibrotic efficacy of statin and protein kinase C inhibitor in hepatic fibrosis.

Journal: American journal of physiology. Gastrointestinal and liver physiology 20100101

Title: Enzastaurin induces H2AX phosphorylation to regulate apoptosis via MAPK signalling in malignant glioma cells.

Journal: European journal of cancer (Oxford, England : 1990) 20100101

Title: Protein kinase Calpha: disease regulator and therapeutic target.

Journal: Trends in pharmacological sciences 20100101

Title: MicroRNA-21 inhibitor sensitizes human glioblastoma cells U251 (PTEN-mutant) and LN229 (PTEN-wild type) to taxol.

Journal: BMC cancer 20100101

Title: Molecular profiling of endometrial malignancies.

Journal: Obstetrics and gynecology international 20100101

Title: Progress on antiangiogenic therapy for patients with malignant glioma.

Journal: Journal of oncology 20100101

Title: Antiangiogenic therapy and mechanisms of tumor resistance in malignant glioma.

Journal: Journal of oncology 20100101

Title: LY294002 may overcome 5-FU resistance via down-regulation of activated p-AKT in Epstein-Barr virus-positive gastric cancer cells.

Journal: BMC cancer 20100101

Title: Cellular responses to Cisplatin-induced DNA damage.

Journal: Journal of nucleic acids 20100101

Title: Signal transduction inhibitor therapy for lymphoma.

Journal: Hematology. American Society of Hematology. Education Program 20100101

Title: A phase II study of oral enzastaurin in patients with metastatic breast cancer previously treated with an anthracycline and a taxane containing regimen.

Journal: Investigational new drugs 20091201

Title: Carboplatin and paclitaxel in combination with oral enzastaurin in advanced ovarian or primary peritoneal cancer: results from a safety lead-in study.

Journal: International journal of gynecological cancer : official journal of the International Gynecological Cancer Society 20091201

Title: Chemotherapy for glioblastoma: current treatment and future perspectives for cytotoxic and targeted agents.

Journal: Anticancer research 20091201

Title: Phase Ib safety and pharmacokinetic evaluation of daily and twice daily oral enzastaurin in combination with pemetrexed in advanced/metastatic cancer.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20090901

Title: Combination of enzastaurin and pemetrexed inhibits cell growth and induces apoptosis of chemoresistant ovarian cancer cells regulating extracellular signal-regulated kinase 1/2 phosphorylation.

Journal: Translational oncology 20090818

Title: Synergistic anti-tumor efficacy of lovastatin and protein kinase C-beta inhibitor in hepatocellular carcinoma.

Journal: Cancer chemotherapy and pharmacology 20090801

Title: Quantitative in situ detection of phosphoproteins in fixed tissues using quantum dot technology.

Journal: The journal of histochemistry and cytochemistry : official journal of the Histochemistry Society 20090701

Title: Enzastaurin shows preclinical antitumor activity against human transitional cell carcinoma and enhances the activity of gemcitabine.

Journal: Molecular cancer therapeutics 20090701

Title: Targeting angiogenesis via a c-Myc/hypoxia-inducible factor-1alpha-dependent pathway in multiple myeloma.

Journal: Cancer research 20090615

Title: Protein kinase C-beta II (PKC-beta II) expression in patients with colorectal cancer.

Journal: International journal of colorectal disease 20090601

Title: Conformationally constrained analogues of diacylglycerol (DAG). 31. Modulation of the biological properties of diacylgycerol lactones (DAG-lactones) containing rigid-rod acyl groups separated from the core lactone by spacer units of different lengths.

Journal: Journal of medicinal chemistry 20090528

Title: Synergistic effect of Sorafenib and Sunitinib with Enzastaurin, a selective protein kinase C inhibitor in renal cell carcinoma cell lines.

Journal: Cancer letters 20090518

Title: A phase I trial of enzastaurin in patients with recurrent gliomas.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20090515

Title: [Role of PKCbeta in the malignant tumors and enzastaurin, a PKCbeta inhibitor].

Journal: Yao xue xue bao = Acta pharmaceutica Sinica 20090501

Title: Perspectives of protein kinase C (PKC) inhibitors as anti-cancer agents.

Journal: Mini reviews in medicinal chemistry 20090401

Title: PKCbeta is essential for the development of chronic lymphocytic leukemia in the TCL1 transgenic mouse model: validation of PKCbeta as a therapeutic target in chronic lymphocytic leukemia.

Journal: Blood 20090319

Title: Molecular targeting of the PKC-beta inhibitor enzastaurin (LY317615) in multiple myeloma involves a coordinated downregulation of MYC and IRF4 expression.

Journal: Hematological oncology 20090301

Title: Protein kinase Cbeta is an effective target for chemoprevention of colon cancer.

Journal: Cancer research 20090215

Title: Targeting PKC: a novel role for beta-catenin in ER stress and apoptotic signaling.

Journal: Blood 20090212

Title: Antiangiogenic drugs in ovarian cancer.

Journal: British journal of cancer 20090113

Title: In vivo/ex vivo and in situ assays used in cancer research: a brief review.

Journal: Toxicologic pathology 20090101

Title: Role of PKCbeta in hepatocellular carcinoma cells migration and invasion in vitro: a potential therapeutic target.

Journal: Clinical & experimental metastasis 20090101

Title: Overview of current and future biologically based targeted therapies in head and neck squamous cell carcinoma.

Journal: Head & neck oncology 20090101

Title: Design of Phase II cancer trials for evaluation of cytostatic/cytotoxic agents.

Journal: Journal of biopharmaceutical statistics 20090101

Title: In Vivo Measurements of Tumor Metabolism and Growth after Administration of Enzastaurin Using Small Animal FDG Positron Emission Tomography.

Journal: Journal of oncology 20090101

Title: Current available therapies and future directions in the treatment of malignant gliomas.

Journal: Biologics : targets & therapy 20090101

Title: MET/PKCbeta expression correlate with metastasis and inhibition is synergistic in lung cancer.

Journal: Journal of carcinogenesis 20090101

Title: Antiproliferative activity of PEP005, a novel ingenol angelate that modulates PKC functions, alone and in combination with cytotoxic agents in human colon cancer cells.

Journal: British journal of cancer 20081202

Title: Exploring multi-targeting strategies for the treatment of gliomas.

Journal: Current opinion in investigational drugs (London, England : 2000) 20081201

Title: Enzastaurin, an inhibitor of PKCbeta, Enhances Antiangiogenic Effects and Cytotoxicity of Radiation against Endothelial Cells.

Journal: Translational oncology 20081201

Title: Waldenstrom macroglobulinemia.

Journal: Cancer letters 20081018

Title: Protein kinase C beta in malignant pleural mesothelioma.

Journal: Anti-cancer drugs 20081001

Title: [Recent therapeutic progress in non-Hodgkin lymphoma: focusing on diffuse large B-cell lymphoma and follicular lymphoma].

Journal: [Rinsho ketsueki] The Japanese journal of clinical hematology 20081001

Title: The heat shock protein antagonist 17-AAG potentiates the activity of enzastaurin against malignant human glioma cells.

Journal: Cancer letters 20080908

Title: Molecular pathways involved in the synergistic interaction of the PKC beta inhibitor enzastaurin with the antifolate pemetrexed in non-small cell lung cancer cells.

Journal: British journal of cancer 20080902

Title: Enzastaurin-induced apoptosis in glioma cells is caspase-dependent and inhibited by BCL-XL.

Journal: Journal of neurochemistry 20080901

Title: Advances in the treatment of monoclonal gammopaties: The emerging role of targeted therapy in plasma cell dyscrasias.

Journal: Biologics : targets & therapy 20080901

Title: Enzastaurin inhibits tumours sensitive and resistant to anti-EGFR drugs.

Journal: British journal of cancer 20080805

Title: The oral protein-kinase C beta inhibitor enzastaurin (LY317615) suppresses signalling through the AKT pathway, inhibits proliferation and induces apoptosis in multiple myeloma cell lines.

Journal: Leukemia & lymphoma 20080701

Title: Current aspects of targeted therapy in head and neck tumors.

Journal: European archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery 20080701

Title: Targeted treatment and new agents in diffuse large B-cell lymphoma.

Journal: Seminars in hematology 20080701

Title: Circulating endothelial cells in oncology: pitfalls and promises.

Journal: British journal of cancer 20080603

Title: Correlations of mRNA expression and in vitro chemosensitivity to enzastaurin in freshly explanted human tumor cells.

Journal: Investigational new drugs 20080601

Title: Enzastaurin renders MCF-7 breast cancer cells sensitive to radiation through reversal of radiation-induced activation of protein kinase C.

Journal: European journal of cancer (Oxford, England : 1990) 20080601

Title: Enzastaurin.

Journal: Expert opinion on investigational drugs 20080601

Title: Sequence-dependent, synergistic antiproliferative and proapoptotic effects of the combination of cytotoxic drugs and enzastaurin, a protein kinase Cbeta inhibitor, in non-small cell lung cancer cells.

Journal: Molecular cancer therapeutics 20080601

Title: Enzastaurin, a protein kinase C beta inhibitor, suppresses signaling through the ribosomal S6 kinase and bad pathways and induces apoptosis in human gastric cancer cells.

Journal: Cancer research 20080315

Title: Involvement of protein kinase C beta-extracellular signal-regulating kinase 1/2/p38 mitogen-activated protein kinase-heat shock protein 27 activation in hepatocellular carcinoma cell motility and invasion.

Journal: Cancer science 20080301

Title: Enzastaurin, an oral serine/threonine kinase inhibitor, as second- or third-line therapy of non-small-cell lung cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20080301

Title: Protein kinase C-beta inhibitor enzastaurin (LY317615.HCI) enhances radiation control of murine breast cancer in an orthotopic model of bone metastasis.

Journal: Investigational new drugs 20080201

Title: A phase II study of enzastaurin, a protein kinase C beta inhibitor, in patients with relapsed or refractory mantle cell lymphoma.

Journal: Annals of oncology : official journal of the European Society for Medical Oncology 20080201

Title: Inhibitors of protein kinase C sensitise multiple myeloma cells to common genotoxic drugs.

Journal: European journal of haematology 20080101

Title: A phase I safety, tolerability, and pharmacokinetic study of enzastaurin combined with capecitabine in patients with advanced solid tumors.

Journal: Anti-cancer drugs 20080101

Title: Protein kinase C isozymes as therapeutic targets for treatment of human cancers.

Journal: Advances in enzyme regulation 20080101

Title: Systemic treatment for advanced (stage IIIb/IV) non-small cell lung cancer: more treatment options; more things to consider. Conclusion.

Journal: The oncologist 20080101

Title: Reduction of HLA-DR+ lymphocytes after treatment with enzastaurin in patients with metastatic thyroid cancer.

Journal: Chemotherapy 20080101

Title: [Protein kinases C: a new cytoplasmic target].

Journal: Bulletin du cancer 20080101

Title: Novel therapies in breast cancer: what is new from ASCO 2008.

Journal: Journal of hematology & oncology 20080101

Title: A Single Institution's Experience with Bevacizumab in Combination with Cytotoxic Chemotherapy in Progressive Malignant Glioma.

Journal: Clinical medicine. Oncology 20080101

Title: Inhibition of protein kinase Cbeta by enzastaurin enhances radiation cytotoxicity in pancreatic cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20071115

Title: Enzastaurin.

Journal: Current opinion in oncology 20071101

Title: Chemoradiotherapy in malignant glioma: standard of care and future directions.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20070910

Title: Safety, tolerability, QTc evaluation, and pharmacokinetics of single and multiple doses of enzastaurin HCl (LY317615), a protein kinase C-beta inhibitor, in healthy subjects.

Journal: Journal of clinical pharmacology 20070901

Title: Enzastaurin, a targeted PKCBeta inhibitor, in relapsed or refractory DLBCL: a promising new strategy based on gene expression signature.

Journal: Current oncology reports 20070901

Title: Phase I pharmacokinetic and pharmacodynamic study of the oral protein kinase C beta-inhibitor enzastaurin in combination with gemcitabine and cisplatin in patients with advanced cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070801

Title: Enzastaurin, a protein kinase Cbeta- selective inhibitor, and its potential application as an anticancer agent in lung cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20070801

Title: Survival improvement in thoracic cancer: progress from the last decade and beyond.

Journal: Lung cancer (Amsterdam, Netherlands) 20070801

Title: Lessons learned in the development of targeted therapy for malignant gliomas.

Journal: Molecular cancer therapeutics 20070701

Title: Protein kinase C inhibitor enzastaurin induces in vitro and in vivo antitumor activity in Waldenstrom macroglobulinemia.

Journal: Blood 20070601

Title: Antitumor activity of enzastaurin (LY317615.HCl) against human cancer cell lines and freshly explanted tumors investigated in in-vitro [corrected] soft-agar cloning experiments.

Journal: Investigational new drugs 20070601

Title: Phase II study of enzastaurin, a protein kinase C beta inhibitor, in patients with relapsed or refractory diffuse large B-cell lymphoma.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20070501

Title: Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl).

Journal: Blood 20070215

Title: Synergistic antiglioma activity of radiotherapy and enzastaurin.

Journal: Annals of neurology 20070201

Title: Role of anti-angiogenesis agents in treating NSCLC: focus on bevacizumab and VEGFR tyrosine kinase inhibitors.

Journal: Current treatment options in oncology 20070201

Title: Retrospective analysis of protein kinase C-beta (PKC-beta) expression in lymphoid malignancies and its association with survival in diffuse large B-cell lymphomas.

Journal: Biology direct 20070101

Title: Inorganic pyrophosphate generation by transforming growth factor-beta-1 is mainly dependent on ANK induction by Ras/Raf-1/extracellular signal-regulated kinase pathways in chondrocytes.

Journal: Arthritis research & therapy 20070101

Title: What is the right dose? The elusive optimal biologic dose in phase I clinical trials.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060901

Title: Phase I dose escalation and pharmacokinetic study of enzastaurin, an oral protein kinase C beta inhibitor, in patients with advanced cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060901

Title: The selective protein kinase C beta inhibitor enzastaurin induces apoptosis in cutaneous T-cell lymphoma cell lines through the AKT pathway.

Journal: The Journal of investigative dermatology 20060701

Title: Enzastaurin (LY317615), a protein kinase Cbeta inhibitor, inhibits the AKT pathway and induces apoptosis in multiple myeloma cell lines.

Journal: Molecular cancer therapeutics 20060701

Title: Development and validation of a drug activity biomarker that shows target inhibition in cancer patients receiving enzastaurin, a novel protein kinase C-beta inhibitor.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20060601

Title: American Association for Cancer Research--97th annual meeting.

Journal: IDrugs : the investigational drugs journal 20060601

Title: Perspectives in central nervous system malignancies.

Journal: IDrugs : the investigational drugs journal 20060601

Title: Protein kinase C-beta as a therapeutic target in breast cancer.

Journal: Seminars in oncology 20060601

Title: Enzastaurin and pemetrexed exert synergistic antitumor activity in thyroid cancer cell lines in vitro.

Journal: International journal of clinical pharmacology and therapeutics 20051201

Title: The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts.

Journal: Cancer research 20050815

Title: The evolution of cancer research and drug discovery at Lilly Research Laboratories.

Journal: Advances in enzyme regulation 20050101

Title: Hypoxia, tumor endothelium, and targets for therapy.

Journal: Advances in experimental medicine and biology 20050101

Title: Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta.

Journal: Bioorganic & medicinal chemistry letters 20030602

Title: Antiangiogenic effects of a protein kinase Cbeta-selective small molecule.

Journal: Cancer chemotherapy and pharmacology 20020101

Title: Graff JR, et al. The protein kinase Cbeta-selective inhibitor, Enzastaurin (LY317615.HCl), suppresses signaling through the AKT pathway, induces apoptosis, and suppresses growth of human colon cancer and glioblastoma xenografts. Cancer Res, 2005, 65(16),

Title: Rovedo MA, et al. Inhibition of glycogen synthase kinase-3 increases the cytotoxicity of enzastaurin. J Invest Dermatol, 2011, 131(7), 1442-1449.

Title: Podar K, et al. Targeting PKC in multiple myeloma: in vitro and in vivo effects of the novel, orally available small-molecule inhibitor enzastaurin (LY317615.HCl). Blood, 2007, 109(4), 1669-1677.

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Tags:170364-57-5 Molecular Formula|170364-57-5 MDL|170364-57-5 SMILES|170364-57-5 Enzastaurin