877399-52-5 | Crizotinib

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$15.00	$10.00
10mg	95%	in stock	$18.00	$12.00
25mg	95%	in stock	$22.00	$15.00
50mg	95%	in stock	$26.00	$18.00
100mg	95%	in stock	$32.00	$22.00
250mg	95%	in stock	$39.00	$27.00
1g	95%	in stock	$89.00	$62.00
5g	95%	in stock	$273.00	$192.00
10g	95%	in stock	$448.00	$314.00
25g	95%	in stock	$782.00	$547.00

Description

• Catalog Number: AB47952
• Chemical Name: Crizotinib
• CAS Number: 877399-52-5
• Molecular Formula: C21H22Cl2FN5O
• Molecular Weight: 450.3367
• MDL Number: MFCD12407409
• SMILES: Nc1ncc(cc1O[C@@H](c1c(Cl)ccc(c1Cl)F)C)c1cnn(c1)C1CCNCC1
• NSC Number: 749005

Computed Properties

• Complexity: 558
• Covalently-Bonded Unit Count: 1
• Defined Atom Stereocenter Count: 1
• Heavy Atom Count: 30
• Hydrogen Bond Acceptor Count: 6
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 5
• XLogP3: 3.7

Upstream Synthesis Route

In chemical synthesis, 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]pyridin-2-amine can be utilized as a key building block for creating novel pharmaceutical compounds. Its unique structure containing a pyrazole and pyridine ring allows for structural modifications that can lead to the development of potent drug candidates. This compound can serve as a versatile intermediate in the synthesis of targeted molecules for various medicinal purposes, including potential applications in drug discovery and development. Its functional groups provide opportunities for further derivatization and optimization to enhance desired biological activities. Whether incorporated directly into the final product or used as a precursor for more complex molecules, this compound plays a vital role in unlocking new chemical entities with therapeutic potential.

Literature

• Cytotoxicity of 34 FDA approved small-molecule kinase inhibitors in primary rat and human hepatocytes.

  Toxicology letters 20180701

• 5-chloro-N4-(2-(isopropylsulfonyl)phenyl)-N2-(2-methoxy-4-(4-((4-methylpiperazin-1-yl)methyl)-1H-1,2,3-triazol-1-yl)phenyl)pyrimidine-2,4-diamine (WY-135), a novel ALK inhibitor, induces cell cycle arrest and apoptosis through inhibiting ALK and its downstream pathways in Karpas299 and H2228 cells.

  Chemico-biological interactions 20180325

• Editor's Highlight: PlacentalDisposition and Effects of Crizotinib: An Ex Vivo Study in the Isolated Dual-Side Perfused Human Cotyledon.

  Toxicological sciences : an official journal of the Society of Toxicology 20170601

• Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.

  Journal of medicinal chemistry 20160526

• Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

  The New England journal of medicine 20160107

• Activity of second-generation ALK inhibitors against crizotinib-resistant mutants in an NPM-ALK model compared to EML4-ALK.

  Cancer medicine 20150701

• PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations.

  Proceedings of the National Academy of Sciences of the United States of America 20150317

• Elucidating mechanisms of toxicity using phenotypic data from primary human cell systems--a chemical biology approach for thrombosis-related side effects.

  International journal of molecular sciences 20150101

• Two novel ALK mutations mediate acquired resistance to the next-generation ALK inhibitor alectinib.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20141115

• Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.

  Journal of medicinal chemistry 20141009

• Selective ALK inhibitor alectinib with potent antitumor activity in models of crizotinib resistance.

  Cancer letters 20140901

• ALK inhibitors in non-small cell lung cancer: crizotinib and beyond.

  Clinical advances in hematology & oncology : H&O 20140701

• Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations.

  Journal of medicinal chemistry 20140612

• The ALK inhibitor ceritinib overcomes crizotinib resistance in non-small cell lung cancer.

  Cancer discovery 20140601

• Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy.

  Nature 20140410

• Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

  Journal of medicinal chemistry 20140227

• Multi-parameter in vitro toxicity testing of crizotinib, sunitinib, erlotinib, and nilotinib in human cardiomyocytes.

  Toxicology and applied pharmacology 20131001

• Identification of potent Yes1 kinase inhibitors using a library screening approach.

  Bioorganic & medicinal chemistry letters 20130801

• Synthesis, structure-activity relationships, and in vivo efficacy of the novel potent and selective anaplastic lymphoma kinase (ALK) inhibitor 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine (LDK378) currently in phase 1 and phase 2 clinical trials.

  Journal of medicinal chemistry 20130725

• Crizotinib for the treatment of non-small-cell lung cancer.

  American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 20130601

• Targeted agents in the third-/fourth-line treatment of patients with advanced (stage III/IV) non-small cell lung cancer (NSCLC).

  Cancer treatment reviews 20130501

• Development and validation of a high-throughput intrinsic ATPase activity assay for the discovery of MEKK2 inhibitors.

  Journal of biomolecular screening 20130401

• Cell culture and Drosophila model systems define three classes of anaplastic lymphoma kinase mutations in neuroblastoma.

  Disease models & mechanisms 20130301

• Prediction of crizotinib-midazolam interaction using the Simcyp population-based simulator: comparison of CYP3A time-dependent inhibition between human liver microsomes versus hepatocytes.

  Drug metabolism and disposition: the biological fate of chemicals 20130201

• Overcoming erlotinib resistance with tailored treatment regimen in patient-derived xenografts from naïve Asian NSCLC patients.

  International journal of cancer 20130115

• Enhancement of the antiproliferative activity of gemcitabine by modulation of c-Met pathway in pancreatic cancer.

  Current pharmaceutical design 20130101

• Anaplastic Lymphoma Kinase (ALK) regulates initiation of transcription of MYCN in neuroblastoma cells.

  Oncogene 20121213

• Isolated central nervous system progression on Crizotinib: an Achilles heel of non-small cell lung cancer with EML4-ALK translocation?

  Cancer biology & therapy 20121201

• Adenocarcinoma of the lung with miliary brain and pulmonary metastases with echinoderm microtubule-associated protein like 4-anaplastic lymphoma kinase translocation treated with crizotinib: a case report.

  Lung cancer (Amsterdam, Netherlands) 20121201

• Antibody targeting of anaplastic lymphoma kinase induces cytotoxicity of human neuroblastoma.

  Oncogene 20121115

• Activation of HER family signaling as a mechanism of acquired resistance to ALK inhibitors in EML4-ALK-positive non-small cell lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20121115

• Hypogonadism related to crizotinib therapy: implications for patient care.

  Cancer 20121101

• Rapid-onset hypogonadism secondary to crizotinib use in men with metastatic nonsmall cell lung cancer.

  Cancer 20121101

• Histologic and cytomorphologic features of ALK-rearranged lung adenocarcinomas.

  Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc 20121101

• ALK alterations in adult renal cell carcinoma: frequency, clinicopathologic features and outcome in a large series of consecutively treated patients.

  Modern pathology : an official journal of the United States and Canadian Academy of Pathology, Inc 20121101

• Targeted therapy for lung cancer.

  Anti-cancer drugs 20121101

• The R1275Q neuroblastoma mutant and certain ATP-competitive inhibitors stabilize alternative activation loop conformations of anaplastic lymphoma kinase.

  The Journal of biological chemistry 20121026

• Crizotinib in ALK-positive lung cancer.

  The Lancet. Oncology 20121001

• Activity and safety of crizotinib in patients with ALK-positive non-small-cell lung cancer: updated results from a phase 1 study.

  The Lancet. Oncology 20121001

• Treatment of ALK-positive non-small cell lung cancer.

  Archives of pathology & laboratory medicine 20121001

• Discovery of a novel class of exquisitely selective mesenchymal-epithelial transition factor (c-MET) protein kinase inhibitors and identification of the clinical candidate 2-(4-(1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)-1H-pyrazol-1-yl)ethanol (PF-04217903) for the treatment of cancer.

  Journal of medicinal chemistry 20120927

• Correlations between the percentage of tumor cells showing an anaplastic lymphoma kinase (ALK) gene rearrangement, ALK signal copy number, and response to crizotinib therapy in ALK fluorescence in situ hybridization-positive nonsmall cell lung cancer.

  Cancer 20120915

• Liquid chromatography-tandem mass spectrometric assay for the ALK inhibitor crizotinib in mouse plasma.

  Journal of chromatography. B, Analytical technologies in the biomedical and life sciences 20120915

• EML4-ALK testing in non-small cell carcinomas of the lung: a review with recommendations.

  Virchows Archiv : an international journal of pathology 20120901

• Discovery of novel 2-aminopyridine-3-carboxamides as c-Met kinase inhibitors.

  Bioorganic & medicinal chemistry 20120901

• Differential protein stability and ALK inhibitor sensitivity of EML4-ALK fusion variants.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

• Variants on a theme: a biomarker of crizotinib response in ALK-positive non-small cell lung cancer?

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

• Identifying and targeting ROS1 gene fusions in non-small cell lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120901

• Targeting ALK: a promising strategy for the treatment of non-small cell lung cancer, non-Hodgkin's lymphoma, and neuroblastoma.

  Targeted oncology 20120901

• [Cavitating nodules in a 40-year-old non-smoking woman: a very particular tumour].

  Revue des maladies respiratoires 20120901

• Histology- and non-histology-driven therapy for treatment of soft tissue sarcomas.

  Annals of oncology : official journal of the European Society for Medical Oncology 20120901

• Echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase-targeted therapy for advanced non-small cell lung cancer: molecular and clinical aspects.

  Cancer science 20120801

• ALK-mutated non-small-cell lung cancer: a new strategy for cancer treatment.

  Lung 20120801

• Disease flare after treatment discontinuation in a patient with EML4-ALK lung cancer and acquired resistance to crizotinib.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120801

• Crizotinib for ALK-rearranged non-small cell lung cancer: a new targeted therapy for a new target.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120715

• The ALK(F1174L) mutation potentiates the oncogenic activity of MYCN in neuroblastoma.

  Cancer cell 20120710

• Crizotinib (PF-02341066) reverses multidrug resistance in cancer cells by inhibiting the function of P-glycoprotein.

  British journal of pharmacology 20120701

• HGF/c-Met pathway is one of the mediators of sunitinib-induced tumor cell type-dependent metastasis.

  Cancer letters 20120701

• Paracrine receptor activation by microenvironment triggers bypass survival signals and ALK inhibitor resistance in EML4-ALK lung cancer cells.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120701

• Inhibitors of the anaplastic lymphoma kinase.

  Expert opinion on investigational drugs 20120701

• Preclinical rationale for use of the clinically available multitargeted tyrosine kinase inhibitor crizotinib in ROS1-translocated lung cancer.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120701

• Anaplastic lymphoma kinase-directed therapy in inflammatory myofibroblastic tumors.

  Current opinion in oncology 20120701

• Autocrine activation of the MET receptor tyrosine kinase in acute myeloid leukemia.

  Nature medicine 20120701

• Antitumor action of the MET tyrosine kinase inhibitor crizotinib (PF-02341066) in gastric cancer positive for MET amplification.

  Molecular cancer therapeutics 20120701

• Personalized medicine and pharmacogenetic biomarkers: progress in molecular oncology testing.

  Expert review of molecular diagnostics 20120701

• Identification of basophils as a major source of hepatocyte growth factor in chronic myeloid leukemia: a novel mechanism of BCR-ABL1-independent disease progression.

  Neoplasia (New York, N.Y.) 20120701

• A molecular dynamics investigation on the crizotinib resistance mechanism of C1156Y mutation in ALK.

  Biochemical and biophysical research communications 20120629

• Targeted therapy for NSCLC: ALK inhibition.

  Journal of oncology pharmacy practice : official publication of the International Society of Oncology Pharmacy Practitioners 20120601

• Histologic subtypes, immunohistochemistry, FISH or molecular screening for the accurate diagnosis of ALK-rearrangement in lung cancer: a comprehensive study of Caucasian non-smokers.

  Lung cancer (Amsterdam, Netherlands) 20120601

• Detection of anaplastic lymphoma kinase (ALK) gene rearrangement in non-small cell lung cancer and related issues in ALK inhibitor therapy: a literature review.

  Molecular diagnosis & therapy 20120601

• Remarkable tumor response to crizotinib in a 14-year-old girl with ALK-positive non-small-cell lung cancer.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120601

• Development of treatment strategies for advanced neuroblastoma.

  International journal of clinical oncology 20120601

• Crizotinib in the treatment of non-small-cell lung cancer.

  Expert opinion on pharmacotherapy 20120601

• ALKoma: a cancer subtype with a shared target.

  Cancer discovery 20120601

• Novel molecular trends in the management of advanced non-small-cell lung cancer.

  Expert review of anticancer therapy 20120601

• Biomarkers that currently affect clinical practice: EGFR, ALK, MET, KRAS.

  Current oncology (Toronto, Ont.) 20120601

• Treatment paradigms for patients with metastatic non-small-cell lung cancer: first-, second-, and third-line.

  Current oncology (Toronto, Ont.) 20120601

• Supportive care treatments for toxicities of anti-egfr and other targeted agents.

  Current oncology (Toronto, Ont.) 20120601

• Discovery of an orally efficacious inhibitor of anaplastic lymphoma kinase.

  Journal of medicinal chemistry 20120524

• Targeting ALK in neuroblastoma--preclinical and clinical advancements.

  Nature reviews. Clinical oncology 20120515

• Promising therapeutic targets in neuroblastoma.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120515

• ALK inhibitor crizotinib combined with intrathecal methotrexate treatment for non-small cell lung cancer with leptomeningeal carcinomatosis.

  Lung cancer (Amsterdam, Netherlands) 20120501

• ALK translocation and crizotinib in non-small cell lung cancer: an evolving paradigm in oncology drug development.

  European journal of cancer (Oxford, England : 1990) 20120501

• Treating ALK-positive lung cancer--early successes and future challenges.

  Nature reviews. Clinical oncology 20120501

• Application of mid-infrared spectroscopy to the development and transfer of a manufacturing process for an active pharmaceutical ingredient.

  Applied spectroscopy 20120501

• [Which platform to support a personalized lung cancer treatment?].

  Bulletin du cancer 20120501

• Novel approaches of chemoradiotherapy in unresectable stage IIIA and stage IIIB non-small cell lung cancer.

  The oncologist 20120501

• Advances in treatment of lung cancer with targeted therapy.

  Archives of pathology & laboratory medicine 20120501

• Discovery pharmacokinetic studies in mice using serial microsampling, dried blood spots and microbore LC-MS/MS.

  Bioanalysis 20120501

• Personalized targeted therapy in advanced non-small cell lung cancer.

  Cleveland Clinic journal of medicine 20120501

• Treating ALK-positive lung cancer in the weeks after the FDA approval of crizotinib.

  The American journal of managed care 20120501

• Treating Anaplastic Lymphoma Kinase-Positive Lung Cancer in the Weeks After the US Food and Drug Administration Approval of Crizotinib.

  Journal of oncology practice 20120501

• Aberrant expression of the transcriptional factor Twist1 promotes invasiveness in ALK-positive anaplastic large cell lymphoma.

  Cellular signalling 20120401

• The biology and clinical features of non-small cell lung cancers with EML4-ALK translocation.

  Current oncology reports 20120401

• The emerging role of ALK inhibitors in the treatment of advanced non-small cell lung cancer.

  Expert opinion on therapeutic targets 20120401

• Astellas' drug discovery strategy: focus on oncology.

  Japanese journal of clinical oncology 20120401

• RNA-Seq mapping and detection of gene fusions with a suffix array algorithm.

  PLoS computational biology 20120401

• ROS1 as a 'druggable' receptor tyrosine kinase: lessons learned from inhibiting the ALK pathway.

  Expert review of anticancer therapy 20120401

• Crizotinib for the treatment of patients with advanced non-small cell lung cancer.

  Drugs of today (Barcelona, Spain : 1998) 20120401

• Recent advances in non-small cell lung cancer biology and clinical management.

  Discovery medicine 20120401

• Redefining clinical trials: the age of personalized medicine.

  Cell 20120316

• The cost-effectiveness of screening lung cancer patients for targeted drug sensitivity markers.

  British journal of cancer 20120313

• ROS1 rearrangements define a unique molecular class of lung cancers.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120310

• Pharmacokinetic/pharmacodynamic modeling of crizotinib for anaplastic lymphoma kinase inhibition and antitumor efficacy in human tumor xenograft mouse models.

  The Journal of pharmacology and experimental therapeutics 20120301

• Mechanisms of resistance to crizotinib in patients with ALK gene rearranged non-small cell lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120301

• LRIG1 modulates cancer cell sensitivity to Smac mimetics by regulating TNFα expression and receptor tyrosine kinase signaling.

  Cancer research 20120301

• Acquired resistance to the ALK inhibitor crizotinib in the absence of an ALK mutation.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120301

• Present status and problems on molecular targeted therapy of cancer.

  Cancer research and treatment : official journal of Korean Cancer Association 20120301

• Mechanisms of acquired crizotinib resistance in ALK-rearranged lung Cancers.

  Science translational medicine 20120208

• Escaping ALK inhibition: mechanisms of and strategies to overcome resistance.

  Science translational medicine 20120208

• Crizotinib (xalkori) for non-small cell lung cancer.

  The Medical letter on drugs and therapeutics 20120206

• Tyrosine kinase gene fusions in cancer: translating mechanisms into targeted therapies.

  Journal of cellular and molecular medicine 20120201

• Dual IHC and FISH testing for ALK gene rearrangement in lung adenocarcinomas in a routine practice: a French study.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20120201

• Coexistence of PIK3CA and other oncogene mutations in lung adenocarcinoma-rationale for comprehensive mutation profiling.

  Molecular cancer therapeutics 20120201

• Cooperation between c-Met and focal adhesion kinase family members in medulloblastoma and implications for therapy.

  Molecular cancer therapeutics 20120201

• Crizotinib: a drug that crystallizes a unique molecular subset of non-small-cell lung cancer.

  Expert review of anticancer therapy 20120201

• Recent advances in pathway-targeted cancer drug therapies emerging from cancer genome analysis.

  Current opinion in genetics & development 20120201

• ROS1 gene rearrangement is identified in NSCLC.

  Cancer discovery 20120201

• Rapid radiographic and clinical improvement after treatment of a MET-amplified recurrent glioblastoma with a mesenchymal-epithelial transition inhibitor.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120120

• Drug approvals 2011: focus on companion diagnostics.

  Journal of the National Cancer Institute 20120118

• ALK gene amplified in most inflammatory breast cancers.

  Journal of the National Cancer Institute 20120118

• Pericyte depletion results in hypoxia-associated epithelial-to-mesenchymal transition and metastasis mediated by met signaling pathway.

  Cancer cell 20120117

• 7,8-dichloro-1-oxo-β-carbolines as a versatile scaffold for the development of potent and selective kinase inhibitors with unusual binding modes.

  Journal of medicinal chemistry 20120112

• Challenges ahead for companion diagnostics.

  Journal of the National Cancer Institute 20120104

• ALK fusion gene positive lung cancer and 3 cases treated with an inhibitor for ALK kinase activity.

  Lung cancer (Amsterdam, Netherlands) 20120101

• More than just an oncogene translocation and a kinase inhibitor: Kevin's story.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20120101

• Rhus verniciflua stokes against advanced cancer: a perspective from the Korean Integrative Cancer Center.

  Journal of biomedicine & biotechnology 20120101

• Crizotinib: in locally advanced or metastatic non-small cell lung cancer.

  Drugs 20120101

• Drug development: portals of discovery.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20120101

• Evaluating translocation gene fusions by SNP array data.

  Cancer informatics 20120101

• Ancillary testing in lung cancer diagnosis.

  Pulmonary medicine 20120101

• Personalized therapy of lung cancer.

  Onkologie 20120101

• STAT3 is activated by JAK2 independent of key oncogenic driver mutations in non-small cell lung carcinoma.

  PloS one 20120101

• KLC1-ALK: a novel fusion in lung cancer identified using a formalin-fixed paraffin-embedded tissue only.

  PloS one 20120101

• ALK-activating homologous mutations in LTK induce cellular transformation.

  PloS one 20120101

• A novel classification of lung cancer into molecular subtypes.

  PloS one 20120101

• Companion diagnostics: changing patient management.

  Ecancermedicalscience 20120101

• Anaplastic lymphoma kinase-positive large B-cell lymphoma: an underrecognized aggressive lymphoma.

  Advances in hematology 20120101

• Internalization and down-regulation of the ALK receptor in neuroblastoma cell lines upon monoclonal antibodies treatment.

  PloS one 20120101

• Novel therapies for aggressive B-cell lymphoma.

  Advances in hematology 20120101

• ALK Signaling and Target Therapy in Anaplastic Large Cell Lymphoma.

  Frontiers in oncology 20120101

• ALK Inhibitors, a Pharmaceutical Perspective.

  Frontiers in oncology 20120101

• A Screening Method for the ALK Fusion Gene in NSCLC.

  Frontiers in oncology 20120101

• [Will targeted therapies replace chemotherapy?].

  Revue medicale de Liege 20120101

• Targeted therapies in sarcomas: challenging the challenge.

  Sarcoma 20120101

• Proof of concept to clinical confirmation: evolving clinical trial designs for targeted agents.

  ISRN oncology 20120101

• [Management of crizotinib, a new individualized treatment].

  Bulletin du cancer 20120101

• Predictive role of computer simulation in assessing signaling pathways of crizotinib-treated A549 lung cancer cells.

  Asian Pacific journal of cancer prevention : APJCP 20120101

• Brentuximab vedotin and crizotinib in anaplastic large-cell lymphoma.

  Cancer journal (Sudbury, Mass.) 20120101

• EML4-ALK-positive non-small cell lung cancer in a patient treated with azathioprine for ulcerative colitis.

  Tumori 20120101

• MET amplification identifies a small and aggressive subgroup of esophagogastric adenocarcinoma with evidence of responsiveness to crizotinib.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20111220

• MET signaling pathway: a rational target for cancer therapy.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20111220

• Activating ALK mutations found in neuroblastoma are inhibited by Crizotinib and NVP-TAE684.

  The Biochemical journal 20111215

• Design, Synthesis and Biological Evaluation of a Series of Novel Axl Kinase Inhibitors.

  ACS medicinal chemistry letters 20111208

• Role of randomized phase III trials in an era of effective targeted therapies.

  Nature reviews. Clinical oncology 20111206

• Role of genotyping in non-small cell lung cancer treatment: current status.

  Drugs 20111203

• ALK mutations conferring differential resistance to structurally diverse ALK inhibitors.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20111201

• New strategies for treatment of ALK-rearranged non-small cell lung cancers.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20111201

• Crizotinib-resistant mutants of EML4-ALK identified through an accelerated mutagenesis screen.

  Chemical biology & drug design 20111201

• Asymptomatic profound sinus bradycardia (heart rate ≤45) in non-small cell lung cancer patients treated with crizotinib.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20111201

• Crizotinib.

  Nature reviews. Drug discovery 20111201

• Incorporation of crizotinib into the NCCN guidelines.

  Journal of the National Comprehensive Cancer Network : JNCCN 20111201

• Crizotinib and testing for ALK.

  Journal of the National Comprehensive Cancer Network : JNCCN 20111201

• Targeted treatment tested as potential cancer cure.

  Nature 20111116

• Differential inhibitor sensitivity of anaplastic lymphoma kinase variants found in neuroblastoma.

  Science translational medicine 20111109

• Larger companies dominate cancer companion diagnostic approvals.

  Nature biotechnology 20111108

• Anaplastic lymphoma kinase as a new target for the treatment of non-small-cell lung cancer.

  Expert review of anticancer therapy 20111101

• Proof of principle for crizotinib in anaplastic lymphoma kinase-positive malignancies was achieved in ALK-positive nonclinical models.

  Molecular cancer therapeutics 20111101

• Treatment for ALK-mutated non-small-cell lung cancer: a new miracle in the research race.

  Clinical & translational oncology : official publication of the Federation of Spanish Oncology Societies and of the National Cancer Institute of Mexico 20111101

• The potential for crizotinib in non-small cell lung cancer: a perspective review.

  Therapeutic advances in medical oncology 20111101

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

• MET tyrosine kinase inhibitor crizotinib (PF-02341066) shows differential antitumor effects in non-small cell lung cancer according to MET alterations.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20111001

• Effect of crizotinib on overall survival in patients with advanced non-small-cell lung cancer harbouring ALK gene rearrangement: a retrospective analysis.

  The Lancet. Oncology 20111001

• Hope without hype: EML4-ALK inhibition for treatment of lung cancer.

  The Lancet. Oncology 20111001

• Emerging importance of ALK in neuroblastoma.

  Seminars in cancer biology 20111001

• Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK).

  Journal of medicinal chemistry 20110922

• 9-substituted 6,6-dimethyl-11-oxo-6,11-dihydro-5H-benzo[b]carbazoles as highly selective and potent anaplastic lymphoma kinase inhibitors.

  Journal of medicinal chemistry 20110922

• A novel ALK secondary mutation and EGFR signaling cause resistance to ALK kinase inhibitors.

  Cancer research 20110915

• Anaplastic lymphoma kinase in human cancer.

  Journal of molecular endocrinology 20110801

• Detection of ALK gene rearrangement in non-small cell lung cancer: a comparison of fluorescence in situ hybridization and chromogenic in situ hybridization with correlation of ALK protein expression.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110801

• Synthesis of an aryloxy oxo pyrimidinone library that displays ALK-selective inhibition.

  Bioorganic & medicinal chemistry letters 20110801

• Differential (18)F-FDG and 3'-deoxy-3'-(18)F-fluorothymidine PET responses to pharmacologic inhibition of the c-MET receptor in preclinical tumor models.

  Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20110801

• Favorable response to crizotinib in three patients with echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase fusion-type oncogene-positive non-small cell lung cancer.

  Cancer science 20110801

• Receptor kinase inhibitors target NSCLC: two antibodies and a small-molecule MET inhibitor.

  BioDrugs : clinical immunotherapeutics, biopharmaceuticals and gene therapy 20110801

• Crizotinib: an anaplastic lymphoma kinase inhibitor.

  Future oncology (London, England) 20110801

• Phase 1 clinical trials for sarcomas: the cutting edge.

  Current opinion in oncology 20110701

• [Molecular targeted drugs against ALK fusions].

  Nihon yakurigaku zasshi. Folia pharmacologica Japonica 20110701

• The orally bioavailable met inhibitor PF-2341066 inhibits osteosarcoma growth and osteolysis/matrix production in a xenograft model.

  Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research 20110601

• [What choice of first-line treatment?].

  Revue de pneumologie clinique 20110601

• [What is the best sequence of treatment for patients with EGFR mutations?].

  Revue de pneumologie clinique 20110601

• [Biomarkers and targeted therapies in non-small cell lung cancer: present and future treatments].

  Revue de pneumologie clinique 20110601

• ALK-targeted therapy for lung cancer: ready for prime time.

  Oncology (Williston Park, N.Y.) 20110601

• CSF concentration of the anaplastic lymphoma kinase inhibitor crizotinib.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20110520

• Pulmonary inflammatory myofibroblastic tumor expressing a novel fusion, PPFIBP1-ALK: reappraisal of anti-ALK immunohistochemistry as a tool for novel ALK fusion identification.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20110515

• Virtual screening and further development of novel ALK inhibitors.

  Bioorganic & medicinal chemistry 20110515

• Therapeutic strategies to overcome crizotinib resistance in non-small cell lung cancers harboring the fusion oncogene EML4-ALK.

  Proceedings of the National Academy of Sciences of the United States of America 20110503

• Activity of crizotinib (PF02341066), a dual mesenchymal-epithelial transition (MET) and anaplastic lymphoma kinase (ALK) inhibitor, in a non-small cell lung cancer patient with de novo MET amplification.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110501

• Genotype-driven therapies for non-small cell lung cancer: focus on EGFR, KRAS and ALK gene abnormalities.

  Therapeutic advances in medical oncology 20110501

• Targeting anaplastic lymphoma kinase in lung cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20110415

• Synthesis and c-Met kinase inhibition of 3,5-disubstituted and 3,5,7-trisubstituted quinolines: identification of 3-(4-acetylpiperazin-1-yl)-5-(3-nitrobenzylamino)-7- (trifluoromethyl)quinoline as a novel anticancer agent.

  Journal of medicinal chemistry 20110414

• Anaplastic lymphoma kinase gene rearrangements in non-small cell lung cancer are associated with prolonged progression-free survival on pemetrexed.

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110401

• Potential therapeutic strategies to overcome acquired resistance to BRAF or MEK inhibitors in BRAF mutant cancers.

  Oncotarget 20110401

• Early accelerated approval for highly targeted cancer drugs.

  The New England journal of medicine 20110324

• NSCLC drug targets acquire new visibility.

  Journal of the National Cancer Institute 20110302

• Prediction of oral pharmacokinetics of cMet kinase inhibitors in humans: physiologically based pharmacokinetic model versus traditional one-compartment model.

  Drug metabolism and disposition: the biological fate of chemicals 20110301

• Crizotinib for EML4-ALK positive lung adenocarcinoma: a hope for the advanced disease? Evaluation of Kwak EL, Bang YJ, Camidge DR, et al. Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer. N Engl J Med 2010;363(18):1693-703.

  Expert opinion on therapeutic targets 20110301

• Personalizing therapy with targeted agents in non-small cell lung cancer.

  Oncotarget 20110301

• New targets in advanced NSCLC: EML4-ALK.

  Clinical advances in hematology & oncology : H&O 20110301

• Crizotinib in anaplastic large-cell lymphoma.

  The New England journal of medicine 20110224

• More on crizotinib.

  The New England journal of medicine 20110224

• More on crizotinib.

  The New England journal of medicine 20110224

• More on crizotinib.

  The New England journal of medicine 20110224

• Distinct interactions between c-Src and c-Met in mediating resistance to c-Src inhibition in head and neck cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20110201

• Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors.

  Cancer research 20110201

• Comparison of 2 cell-based phosphoprotein assays to support screening and development of an ALK inhibitor.

  Journal of biomolecular screening 20110201

• Kinetic control of protonation in electrospray ionization.

  Journal of the American Society for Mass Spectrometry 20110201

• Summary of presentations from the 46th Annual Meeting of the American Society of Clinical Oncology: focus on non-small cell lung cancer (2010).

  Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20110101

• MET inhibitors: translating from bench to bedside.

  The Lancet. Oncology 20110101

• Gastrointestinal Mesenchymal Neoplasms other than Gastrointestinal Stromal Tumors: Focusing on Their Molecular Aspects.

  Pathology research international 20110101

• Targeted therapies and other agents as first-line maintenance and beyond: particular benefit in pulmonary adenocarcinoma patients.

  Current medicinal chemistry 20110101

• Wnt signaling and colon carcinogenesis: beyond APC.

  Journal of carcinogenesis 20110101

• Novel targeted therapeutics: inhibitors of MDM2, ALK and PARP.

  Journal of hematology & oncology 20110101

• Target therapies in lung cancer.

  Journal of biomedicine & biotechnology 20110101

• Inhibitor-sensitive FGFR1 amplification in human non-small cell lung cancer.

  PloS one 20110101

• Advances in fine needle aspiration cytology for the diagnosis of pulmonary carcinoma.

  Pathology research international 20110101

• From the bench to bedside: biological and methodology considerations for the future of companion diagnostics in nonsmall cell lung cancer.

  Pathology research international 20110101

• Transglutaminase 2 as an independent prognostic marker for survival of patients with non-adenocarcinoma subtype of non-small cell lung cancer.

  Molecular cancer 20110101

• Resistance to cancer treatment: the role of somatic genetic events and the challenges for targeted therapies.

  Frontiers in pharmacology 20110101

• ALK and NSCLC: Targeted therapy with ALK inhibitors.

  F1000 medicine reports 20110101

• Signatures of drug sensitivity in nonsmall cell lung cancer.

  International journal of proteomics 20110101

• Spectrum of oncogenic driver mutations in lung adenocarcinomas from East Asian never smokers.

  PloS one 20110101

• Crizotinib: a novel and first-in-class multitargeted tyrosine kinase inhibitor for the treatment of anaplastic lymphoma kinase rearranged non-small cell lung cancer and beyond.

  Drug design, development and therapy 20110101

• New drug therapies, dedicated specialists and desperately-ill patients-but who will fly the flag for service developments in lung cancer as NHS budgets come under pressure?

  Ecancermedicalscience 20110101

• An update on the management of peripheral T-cell lymphoma and emerging treatment options.

  Journal of blood medicine 20110101

• Personalized therapy for non-small cell lung cancer: which drug for which patient?

  Seminars in thoracic and cardiovascular surgery 20110101

• Anaplastic Lymphoma Kinase: role in specific tumours, and development of small molecule inhibitors for cancer therapy.

  Cancer letters 20101228

• The neuroblastoma-associated F1174L ALK mutation causes resistance to an ALK kinase inhibitor in ALK-translocated cancers.

  Cancer research 20101215

• ALK inhibition for non-small cell lung cancer: from discovery to therapy in record time.

  Cancer cell 20101214

• New drugs in advanced non-small-cell lung cancer: searching for the correct clinical development.

  Expert opinion on investigational drugs 20101201

• Parameters for individualizing systemic therapy in non-small cell lung cancer.

  Drug resistance updates : reviews and commentaries in antimicrobial and anticancer chemotherapy 20101201

• Rapid and dramatic radiographic and clinical response to an ALK inhibitor (crizotinib, PF02341066) in an ALK translocation-positive patient with non-small cell lung cancer.

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

• Trial watch: success for crizotinib in ALK-driven cancer.

  Nature reviews. Drug discovery 20101201

• Crizotinib, a small-molecule dual inhibitor of the c-Met and ALK receptor tyrosine kinases.

  Current opinion in investigational drugs (London, England : 2000) 20101201

• [Following communications made at American Society of Clinical Oncology 2010, what will change our practice? The point of view of the editorial board of Bulletin du Cancer].

  Bulletin du cancer 20101201

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

  Chemistry & biology 20101124

• Anaplastic lymphoma kinase inhibition in non-small-cell lung cancer.

  The New England journal of medicine 20101028

• Crizotinib in ALK-rearranged inflammatory myofibroblastic tumor.

  The New England journal of medicine 20101028

• EML4-ALK mutations in lung cancer that confer resistance to ALK inhibitors.

  The New England journal of medicine 20101028

• Crizotinib--latest champion in the cancer wars?

  The New England journal of medicine 20101028

• Exciting new targets in lung cancer therapy: ALK, IGF-1R, HDAC, and Hh.

  Current treatment options in oncology 20100601

• Gender specific drug metabolism of PF-02341066 in rats--role of sulfoconjugation.

  Current drug metabolism 20100501

• Discovery of 6-benzyloxyquinolines as c-Met selective kinase inhibitors.

  Bioorganic & medicinal chemistry letters 20100215

• Acquired resistance of non-small cell lung cancer cells to MET kinase inhibition is mediated by a switch to epidermal growth factor receptor dependency.

  Cancer research 20100215

• An orally available small-molecule inhibitor of c-Met, PF-2341066, reduces tumor burden and metastasis in a preclinical model of ovarian cancer metastasis.

  Neoplasia (New York, N.Y.) 20100101

• Efficacy of c-Met inhibitor for advanced prostate cancer.

  BMC cancer 20100101

• Deciding priorities in Pharma.

  Breast cancer research : BCR 20100101

• HGF and c-Met participate in paracrine tumorigenic pathways in head and neck squamous cell cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20090601

• An orally available small-molecule inhibitor of c-Met, PF-2341066, exhibits cytoreductive antitumor efficacy through antiproliferative and antiangiogenic mechanisms.

  Cancer research 20070501