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187724-61-4,MFCD09970842
Catalog No.:AA00BBFJ

187724-61-4 | PKI 166

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1mg
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5mg
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$172.00   $120.00
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10mg
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00BBFJ
Chemical Name:
PKI 166
CAS Number:
187724-61-4
Molecular Formula:
C20H18N4O
Molecular Weight:
330.3831
MDL Number:
MFCD09970842
SMILES:
Oc1ccc(cc1)c1[nH]c2c(c1)c(ncn2)N[C@@H](c1ccccc1)C
Properties
Computed Properties
 
Complexity:
420  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Heavy Atom Count:
25  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
3  
Rotatable Bond Count:
4  
XLogP3:
4.2  

Literature

Title: Synthesis and in vitro EGFR (ErbB1) tyrosine kinase inhibitory activity of 4-N-substituted 6-aryl-7H-pyrrolo[2,3-d]pyrimidine-4-amines.

Journal: European journal of medicinal chemistry 20111201

Title: Liver X receptors as regulators of macrophage inflammatory and metabolic pathways.

Journal: Biochimica et biophysica acta 20110801

Title: Inhibition of the epidermal growth factor receptor preserves podocytes and attenuates albuminuria in experimental diabetic nephropathy.

Journal: Nephrology (Carlton, Vic.) 20110801

Title: Axonal neuregulin 1 type III activates NF-kappaB in Schwann cells during myelin formation.

Journal: The Journal of biological chemistry 20100528

Title: Regeneration of human epidermis on acellular dermis is impeded by small-molecule inhibitors of EGF receptor tyrosine kinase.

Journal: Archives of dermatological research 20081001

Title: Phosphorylated epidermal growth factor receptor on tumor-associated endothelial cells is a primary target for therapy with tyrosine kinase inhibitors.

Journal: Neoplasia (New York, N.Y.) 20080501

Title: Pharmacology of epidermal growth factor inhibitors.

Journal: The International journal of biological markers 20070101

Title: Tyrosine kinases: maiming myelin in leprosy.

Journal: Nature medicine 20060801

Title: ErbB2 receptor tyrosine kinase signaling mediates early demyelination induced by leprosy bacilli.

Journal: Nature medicine 20060801

Title: Phase I and pharmacologic study of PKI166, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20051001

Title: Antitumor activity of HER-2 inhibitors.

Journal: Cancer letters 20050908

Title: Epidermal growth factor inhibition in solid tumours.

Journal: Expert opinion on biological therapy 20050901

Title: Microanatomy of axon/glial signaling during Wallerian degeneration.

Journal: The Journal of neuroscience : the official journal of the Society for Neuroscience 20050330

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

Journal: Seminars in oncology 20050201

Title: Monitoring antiproliferative responses to kinase inhibitor therapy in mice with 3'-deoxy-3'-18F-fluorothymidine PET.

Journal: Journal of nuclear medicine : official publication, Society of Nuclear Medicine 20050101

Title: Epidermal growth factor receptor tyrosine kinase inhibitor does not improve paclitaxel effect in an orthotopic mouse model of lung cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20041215

Title: Relationship between antiapoptotic molecules and metastatic potency and the involvement of DNA-dependent protein kinase in the chemosensitization of metastatic human cancer cells by epidermal growth factor receptor blockade.

Journal: The Journal of pharmacology and experimental therapeutics 20041201

Title: Cooperation between fibroblast growth factor receptor-4 and ErbB2 in regulation of cyclin D1 translation.

Journal: The Journal of biological chemistry 20041126

Title: Hepatic transport of PKI166, an epidermal growth factor receptor kinase inhibitor of the pyrrolo-pyrimidine class, and its main metabolite, ACU154.

Journal: Drug metabolism and disposition: the biological fate of chemicals 20041101

Title: Epidermal growth factor receptor inhibition attenuates early kidney enlargement in experimental diabetes.

Journal: Kidney international 20041101

Title: HER2/neu kinase-dependent modulation of androgen receptor function through effects on DNA binding and stability.

Journal: Cancer cell 20041101

Title: Epidermal growth factor receptor inhibition promotes desmosome assembly and strengthens intercellular adhesion in squamous cell carcinoma cells.

Journal: The Journal of biological chemistry 20040827

Title: Simultaneous blockade of platelet-derived growth factor-receptor and epidermal growth factor-receptor signaling and systemic administration of paclitaxel as therapy for human prostate cancer metastasis in bone of nude mice.

Journal: Cancer research 20040615

Title: Hypoxia increases resistance of human pancreatic cancer cells to apoptosis induced by gemcitabine.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20040401

Title: Novel radiosensitizers for locally advanced epithelial tumors: inhibition of the PI3K/Akt survival pathway in tumor cells and in tumor-associated endothelial cells as a novel treatment strategy?

Journal: International journal of radiation oncology, biology, physics 20040201

Title: Bioassay using epidermal keratinocytes to determine phosphorylation status of the epidermal growth factor receptor in distant neoplasms.

Journal: International journal of oncology 20040101

Title: [Targeting of epidermal growth factor receptor and applications in ORL cancer].

Journal: Bulletin du cancer 20031101

Title: Renal cell carcinoma bone metastasis: epidermal growth factor receptor targeting.

Journal: Clinical orthopaedics and related research 20031001

Title: Clinical studies with non-iressa EGFR tyrosine kinase inhibitors.

Journal: Lung cancer (Amsterdam, Netherlands) 20030801

Title: Epidermal growth factor receptor blockade potentiates apoptosis mediated by Paclitaxel and leads to prolonged survival in a murine model of oral cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030801

Title: Inhibition of zebrafish epidermal growth factor receptor activity results in cardiovascular defects.

Journal: Mechanisms of development 20030701

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

Journal: Journal of the National Cancer Institute 20030618

Title: Blockade of epidermal growth factor receptor signaling leads to inhibition of renal cell carcinoma growth in the bone of nude mice.

Journal: Cancer research 20030601

Title: Tyrosine kinases as targets in cancer therapy - successes and failures.

Journal: Expert opinion on therapeutic targets 20030401

Title: Blockade of epidermal growth factor receptor signaling in tumor cells and tumor-associated endothelial cells for therapy of androgen-independent human prostate cancer growing in the bone of nude mice.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20030301

Title: Blockade of the epidermal growth factor receptor signaling inhibits angiogenesis leading to regression of human renal cell carcinoma growing orthotopically in nude mice.

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

Title: Blockade of epidermal growth factor receptor signaling on tumor cells and tumor-associated endothelial cells for therapy of human carcinomas.

Journal: The American journal of pathology 20020901

Title: The efficacy of ErbB receptor-targeted anticancer therapeutics is influenced by the availability of epidermal growth factor-related peptides.

Journal: Cancer research 20020601

Title: Blockade of vascular endothelial growth factor receptor and epidermal growth factor receptor signaling for therapy of metastatic human pancreatic cancer.

Journal: Cancer research 20020401

Title: HER-targeted tyrosine-kinase inhibitors.

Journal: Oncology 20020101

Title: Anticancer therapy targeting the erbB family of receptor tyrosine kinases.

Journal: Seminars in oncology 20011001

Title: Mammary glands reconstituted with Neu/ErbB2 transformed HC11 cells provide a novel orthotopic tumor model for testing anti-cancer agents.

Journal: Oncogene 20010906

Title: Optimization for the blockade of epidermal growth factor receptor signaling for therapy of human pancreatic carcinoma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20010801

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