257933-82-7 | Pelitinib

Packsize	Purity	Availability	Price	Discounted Price
1mg	95%	in stock	$48.00	$33.00
25mg	95%	in stock	$74.00	$52.00
100mg	95%	in stock	$160.00	$112.00
250mg	95%	in stock	$315.00	$221.00
1g	95%	in stock	$844.00	$591.00
5g	95%	in stock	$2,514.00	$1,760.00

Description

• Catalog Number: AD54879
• Chemical Name: Pelitinib
• CAS Number: 257933-82-7
• Molecular Formula: C24H23ClFN5O2
• Molecular Weight: 467.9231
• MDL Number: MFCD09837868
• SMILES: CCOc1cc2ncc(c(c2cc1NC(=O)/C=C/CN(C)C)Nc1ccc(c(c1)Cl)F)C#N
• NSC Number: 729742

Computed Properties

• Complexity: 729
• Covalently-Bonded Unit Count: 1
• Defined Bond Stereocenter Count: 1
• Heavy Atom Count: 33
• Hydrogen Bond Acceptor Count: 7
• Hydrogen Bond Donor Count: 2
• Rotatable Bond Count: 8
• XLogP3: 4.5

Literature

• Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family.

  Journal of medicinal chemistry 20160908

• Phase I study of temsirolimus in combination with EKB-569 in patients with advanced solid tumors.

  Investigational new drugs 20121001

• Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance.

  Biochemical pharmacology 20120801

• Differential action of small molecule HER kinase inhibitors on receptor heterodimerization: therapeutic implications.

  International journal of cancer 20120701

• Novel EGFR-TK inhibitor EKB-569 inhibits hepatocellular carcinoma cell proliferation by AKT and MAPK pathways.

  Journal of Korean medical science 20111201

• The PI3 kinase/mTOR blocker NVP-BEZ235 overrides resistance against irreversible ErbB inhibitors in breast cancer cells.

  Breast cancer research and treatment 20110901

• Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.

  European journal of medicinal chemistry 20110601

• Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.

  Journal of medicinal chemistry 20110310

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

  PloS one 20110101

• Development of a new epidermal growth factor receptor positron emission tomography imaging agent based on the 3-cyanoquinoline core: synthesis and biological evaluation.

  Bioorganic & medicinal chemistry 20100915

• Irreversible pan-ErbB tyrosine kinase inhibitors and breast cancer: current status and future directions.

  Cancer treatment reviews 20091201

• A phase I study of EKB-569 in combination with capecitabine in patients with advanced colorectal cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20080901

• Redesigning kinase inhibitors to enhance specificity.

  Journal of medicinal chemistry 20080828

• The development of HKI-272 and related compounds for the treatment of cancer.

  Archiv der Pharmazie 20080801

• Chronic pharmacologic inhibition of EGFR leads to cardiac dysfunction in C57BL/6J mice.

  Toxicology and applied pharmacology 20080501

• Towards predictive inhibitor design for the EGFR autophosphorylation activity.

  European journal of medicinal chemistry 20080401

• Phase I pharmacokinetic/pharmacodynamic study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor tyrosine kinase, in combination with irinotecan, 5-fluorouracil, and leucovorin (FOLFIRI) in first-line treatment of patients with metastatic colorectal cancer.

  Clinical cancer research : an official journal of the American Association for Cancer Research 20080101

• A quantitative analysis of kinase inhibitor selectivity.

  Nature biotechnology 20080101

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

  Journal of receptor and signal transduction research 20080101

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

  Bioorganic & medicinal chemistry 20070601

• In-Cell Western analysis of Helicobacter pylori-induced phosphorylation of extracellular-signal related kinase via the transactivation of the epidermal growth factor receptor.

  Microbes and infection 20070601

• Second-generation epidermal growth factor receptor tyrosine kinase inhibitors in non-small cell lung cancer.

  The oncologist 20070301

• Pharmacology of epidermal growth factor inhibitors.

  The International journal of biological markers 20070101

• Is there a role for the irreversible epidermal growth factor receptor inhibitor EKB-569 in the treatment of cancer? A mutation-driven question.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060520

• Phase I study of EKB-569, an irreversible inhibitor of the epidermal growth factor receptor, in patients with advanced solid tumors.

  Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20060520

• EKB-569, a new irreversible epidermal growth factor receptor tyrosine kinase inhibitor, with clinical activity in patients with non-small cell lung cancer with acquired resistance to gefitinib.

  Lung cancer (Amsterdam, Netherlands) 20060301

• Recent developments related to the EGFR as a target for cancer chemotherapy.

  Current opinion in pharmacology 20050801

• Small molecules with EGFR-TK inhibitor activity.

  Current drug targets 20050501

• A small molecule-kinase interaction map for clinical kinase inhibitors.

  Nature biotechnology 20050301

• Optimization of 6,7-disubstituted-4-(arylamino)quinoline-3-carbonitriles as orally active, irreversible inhibitors of human epidermal growth factor receptor-2 kinase activity.

  Journal of medicinal chemistry 20050224

• The epidermal growth factor receptor as a target for colorectal cancer therapy.

  Seminars in oncology 20050201

• Epidermal growth factor receptor tyrosine kinase inhibition is not protective in PCK rats.

  Kidney international 20041101

• Syntheses and EGFR kinase inhibitory activity of 6-substituted-4-anilino [1,7] and [1,8] naphthyridine-3-carbonitriles.

  Bioorganic & medicinal chemistry letters 20040322

• Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes.

  Molecular cancer therapeutics 20040101

• Combination treatment of PKD utilizing dual inhibition of EGF-receptor activity and ligand bioavailability.

  Kidney international 20031001

• Clinical studies with non-iressa EGFR tyrosine kinase inhibitors.

  Lung cancer (Amsterdam, Netherlands) 20030801

• Developing inhibitors of the epidermal growth factor receptor for cancer treatment.

  Journal of the National Cancer Institute 20030618

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

  Journal of medicinal chemistry 20030102

• Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.

  Bioorganic & medicinal chemistry letters 20021021