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477575-56-7,MFCD07772270
Catalog No.:AA00DB4G

477575-56-7 | PHA-665752

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1mg
99%
in stock  
$44.00   $31.00
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5mg
99%
in stock  
$110.00   $77.00
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10mg
99%
in stock  
$163.00   $114.00
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50mg
98%
in stock  
$702.00   $492.00
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA00DB4G
Chemical Name:
PHA-665752
CAS Number:
477575-56-7
Molecular Formula:
C32H34Cl2N4O4S
Molecular Weight:
641.6078
MDL Number:
MFCD07772270
SMILES:
O=C1Nc2c(/C/1=C/c1[nH]c(c(c1C)C(=O)N1CCC[C@@H]1CN1CCCC1)C)cc(cc2)S(=O)(=O)Cc1c(Cl)cccc1Cl
Properties
Properties
 
BP:
890.17°C at 760 mmHg  
Form:
Solid  
Storage:
Keep in dry area;2-8℃;  

Computed Properties
 
Complexity:
1180  
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
1  
Defined Bond Stereocenter Count:
1  
Heavy Atom Count:
43  
Hydrogen Bond Acceptor Count:
5  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
7  
XLogP3:
5  

Literature

Title: Ochratoxin A activates opposing c-MET/PI3K/Akt and MAPK/ERK 1-2 pathways in human proximal tubule HK-2 cells.

Journal: Archives of toxicology 20150801

Title: Proteinase-activated receptor 2 (PAR(2)) in cholangiocarcinoma (CCA) cells: effects on signaling and cellular level.

Journal: Histochemistry and cell biology 20121201

Title: Macroporous hydrogel micropillars for quantifying Met kinase activity in cancer cell lysates.

Journal: The Analyst 20120907

Title: Association of activated c-Met with NRAS-mutated human melanomas.

Journal: International journal of cancer 20120715

Title: Targeting MET by tyrosine kinase inhibitor suppresses growth and invasion of nasopharyngeal carcinoma cell lines.

Journal: Pathology oncology research : POR 20120401

Title: A preclinical algorithm of soluble surrogate biomarkers that correlate with therapeutic inhibition of the MET oncogene in gastric tumors.

Journal: International journal of cancer 20120315

Title: MET activation mediates resistance to lapatinib inhibition of HER2-amplified gastric cancer cells.

Journal: Molecular cancer therapeutics 20120301

Title: MET inhibition in tumor cells by PHA665752 impairs homologous recombination repair of DNA double strand breaks.

Journal: International journal of cancer 20120201

Title: c-Met inhibitor synergizes with tumor necrosis factor-related apoptosis-induced ligand to induce papillary thyroid carcinoma cell death.

Journal: Molecular medicine (Cambridge, Mass.) 20120101

Title: Coexpression of activated c-Met and death receptor 5 predicts better survival in colorectal carcinoma.

Journal: The American journal of pathology 20111201

Title: Comprehensive analysis of kinase inhibitor selectivity.

Journal: Nature biotechnology 20111030

Title: PTEN reconstitution alters glioma responses to c-Met pathway inhibition.

Journal: Anti-cancer drugs 20111001

Title: 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: Journal of medicinal chemistry 20110922

Title: MET phosphorylation predicts poor outcome in small cell lung carcinoma and its inhibition blocks HGF-induced effects in MET mutant cell lines.

Journal: British journal of cancer 20110906

Title: c-Met represents a potential therapeutic target for personalized treatment in hepatocellular carcinoma.

Journal: Hepatology (Baltimore, Md.) 20110902

Title: Coactivation of receptor tyrosine kinases in malignant mesothelioma as a rationale for combination targeted therapy.

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

Title: Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer.

Journal: Journal of the National Cancer Institute 20110420

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

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

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

Journal: Cancer research 20110201

Title: HGF/c-Met pathway has a prominent role in mediating antiapoptotic signals through AKT in epithelial ovarian carcinoma.

Journal: Laboratory investigation; a journal of technical methods and pathology 20110101

Title: Antitumor activity of SNX-2112, a synthetic heat shock protein-90 inhibitor, in MET-amplified tumor cells with or without resistance to selective MET Inhibition.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110101

Title: Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma.

Journal: Neoplasia (New York, N.Y.) 20110101

Title: Involvement of c-Met- and phosphatidylinositol 3-kinase dependent pathways in arsenite-induced downregulation of catalase in hepatoma cells.

Journal: Biological & pharmaceutical bulletin 20110101

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

Journal: Chemistry & biology 20101124

Title: MET and KRAS gene amplification mediates acquired resistance to MET tyrosine kinase inhibitors.

Journal: Cancer research 20101001

Title: Molecular predictors of sensitivity to the MET inhibitor PHA665752 in lung carcinoma cells.

Journal: Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer 20100901

Title: Identification of c-Src as a potential therapeutic target for gastric cancer and of MET activation as a cause of resistance to c-Src inhibition.

Journal: Molecular cancer therapeutics 20100501

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

Journal: Cancer research 20100215

Title: Scatter factor protects tumor cells against apoptosis caused by TRAIL.

Journal: Anti-cancer drugs 20100101

Title: Efficacy of c-Met inhibitor for advanced prostate cancer.

Journal: BMC cancer 20100101

Title: N-(4-(6,7-Disubstituted-quinolin-4-yloxy)-3-fluorophenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20091201

Title: met oncogene activation qualifies spontaneous canine osteosarcoma as a suitable pre-clinical model of human osteosarcoma.

Journal: The Journal of pathology 20090701

Title: N-(3-fluoro-4-(2-arylthieno[3,2-b]pyridin-7-yloxy)phenyl)-2-oxo-3-phenylimidazolidine-1-carboxamides: a novel series of dual c-Met/VEGFR2 receptor tyrosine kinase inhibitors.

Journal: Bioorganic & medicinal chemistry letters 20090301

Title: PHA665752, a small-molecule inhibitor of c-Met, inhibits hepatocyte growth factor-stimulated migration and proliferation of c-Met-positive neuroblastoma cells.

Journal: BMC cancer 20090101

Title: Role of non-receptor and receptor tyrosine kinases (TKs) in the antitumor action of alpha-difluoromethylornithine (DFMO) in breast cancer cells.

Journal: Breast cancer research and treatment 20081101

Title: HER kinase activation confers resistance to MET tyrosine kinase inhibition in MET oncogene-addicted gastric cancer cells.

Journal: Molecular cancer therapeutics 20081101

Title: Small molecule c-MET inhibitor PHA665752: effect on cell growth and motility in papillary thyroid carcinoma.

Journal: Head & neck 20080801

Title: Hepatocyte growth factor and c-Met promote dendritic maturation during hippocampal neuron differentiation via the Akt pathway.

Journal: Cellular signalling 20080501

Title: Hepatocyte growth factor promotes migration of human myeloma cells.

Journal: Haematologica 20080401

Title: An in vivo model of Met-driven lymphoma as a tool to explore the therapeutic potential of Met inhibitors.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20080401

Title: A selective small molecule inhibitor of c-Met, PHA-665752, reverses lung premalignancy induced by mutant K-ras.

Journal: Molecular cancer therapeutics 20080401

Title: Hepatocyte growth factor enhances death receptor-induced apoptosis by up-regulating DR5.

Journal: BMC cancer 20080101

Title: MET amplification leads to gefitinib resistance in lung cancer by activating ERBB3 signaling.

Journal: Science (New York, N.Y.) 20070518

Title: A selective small molecule inhibitor of c-Met, PHA665752, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.

Journal: Cancer research 20070415

Title: TFE3 fusions activate MET signaling by transcriptional up-regulation, defining another class of tumors as candidates for therapeutic MET inhibition.

Journal: Cancer research 20070201

Title: Inhibition of the met receptor in mesothelioma.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20051115

Title: A selective small molecule c-MET Inhibitor, PHA665752, cooperates with rapamycin.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20050315

Title: A selective c-met inhibitor blocks an autocrine hepatocyte growth factor growth loop in ANBL-6 cells and prevents migration and adhesion of myeloma cells.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20041001

Title: A selective small molecule inhibitor of c-Met kinase inhibits c-Met-dependent phenotypes in vitro and exhibits cytoreductive antitumor activity in vivo.

Journal: Cancer research 20031101

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