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877399-52-5 | 3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]pyridin-2-amine
CAS No: 877399-52-5 Catalog No: AG0036BC MDL No:MFCD12407409
Product Description
Catalog Number:
AG0036BC
Chemical Name:
3-[(1R)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]pyridin-2-amine
CAS Number:
877399-52-5
Molecular Formula:
C21H22Cl2FN5O
Molecular Weight:
450.3367
MDL Number:
MFCD12407409
IUPAC Name:
3-[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine
InChI:
InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1
InChI Key:
KTEIFNKAUNYNJU-GFCCVEGCSA-N
SMILES:
Nc1ncc(cc1O[C@@H](c1c(Cl)ccc(c1Cl)F)C)c1cnn(c1)C1CCNCC1
UNII:
53AH36668S
NSC Number:
749005
Properties
Complexity:
558
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1
Defined Atom Stereocenter Count:
1
Defined Bond Stereocenter Count:
0
Exact Mass:
449.119g/mol
Formal Charge:
0
Heavy Atom Count:
30
Hydrogen Bond Acceptor Count:
6
Hydrogen Bond Donor Count:
2
Isotope Atom Count:
0
Molecular Weight:
450.339g/mol
Monoisotopic Mass:
449.119g/mol
Rotatable Bond Count:
5
Topological Polar Surface Area:
78A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
3.7
Literature
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| 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 |
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