477575-56-7 | PHA-665752

Packsize	Purity	Availability	Price	Discounted Price
1mg	99%	in stock	$41.00	$29.00
5mg	≥98%	in stock	$99.00	$70.00
10mg	99%	in stock	$153.00	$107.00
25mg	95%	in stock	$329.00	$230.00
50mg	95%	in stock	$522.00	$365.00
100mg	95%	in stock	$843.00	$590.00

Description

• Catalog Number: AG20844
• 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

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

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

  Archives of toxicology 20150801

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

  Histochemistry and cell biology 20121201

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

  The Analyst 20120907

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

  International journal of cancer 20120715

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

  Pathology oncology research : POR 20120401

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

  International journal of cancer 20120315

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

  Molecular cancer therapeutics 20120301

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

  International journal of cancer 20120201

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

  Molecular medicine (Cambridge, Mass.) 20120101

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

  The American journal of pathology 20111201

• Comprehensive analysis of kinase inhibitor selectivity.

  Nature biotechnology 20111030

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

  Anti-cancer drugs 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

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

  British journal of cancer 20110906

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

  Hepatology (Baltimore, Md.) 20110902

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

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

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

  Journal of the National Cancer Institute 20110420

• 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

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

  Laboratory investigation; a journal of technical methods and pathology 20110101

• 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.

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

• Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma.

  Neoplasia (New York, N.Y.) 20110101

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

  Biological & pharmaceutical bulletin 20110101

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

  Chemistry & biology 20101124

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

  Cancer research 20101001

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

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

• 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.

  Molecular cancer therapeutics 20100501

• 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

• Scatter factor protects tumor cells against apoptosis caused by TRAIL.

  Anti-cancer drugs 20100101

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

  BMC cancer 20100101

• 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.

  Bioorganic & medicinal chemistry letters 20091201

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

  The Journal of pathology 20090701

• 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.

  Bioorganic & medicinal chemistry letters 20090301

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

  BMC cancer 20090101

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

  Breast cancer research and treatment 20081101

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

  Molecular cancer therapeutics 20081101

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

  Head & neck 20080801

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

  Cellular signalling 20080501

• Hepatocyte growth factor promotes migration of human myeloma cells.

  Haematologica 20080401

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

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

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

  Molecular cancer therapeutics 20080401

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

  BMC cancer 20080101

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

  Science (New York, N.Y.) 20070518

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

  Cancer research 20070415

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

  Cancer research 20070201

• Inhibition of the met receptor in mesothelioma.

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

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

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

• 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.

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

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

  Cancer research 20031101