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company name :
Tocris Bioscience
product type :
chemical
product name :
PHA 665752
catalog :
2693/10
quantity :
10 mg (also 50 mg)
price :
416 USD
more info or order :
citations: 34
Reference
Choi W, Lee J, Lee J, Lee S, Kim S. Hepatocyte Growth Factor Regulates Macrophage Transition to the M2 Phenotype and Promotes Murine Skeletal Muscle Regeneration. Front Physiol. 2019;10:914 pubmed publisher
Giménez Xavier P, Pros E, Bonastre E, Moran S, Aza A, Grana O, et al. Genomic and Molecular Screenings Identify Different Mechanisms for Acquired Resistance to MET Inhibitors in Lung Cancer Cells. Mol Cancer Ther. 2017;16:1366-1376 pubmed publisher
Rycaj K, Cho E, Liu X, Chao H, Liu B, Li Q, et al. Longitudinal tracking of subpopulation dynamics and molecular changes during LNCaP cell castration and identification of inhibitors that could target the PSA-/lo castration-resistant cells. Oncotarget. 2016;7:14220-40 pubmed publisher
Valente S, Ciavarella C, Pasanisi E, Ricci F, Stella A, Pasquinelli G. Hepatocyte Growth Factor Effects on Mesenchymal Stem Cells Derived from Human Arteries: A Novel Strategy to Accelerate Vascular Ulcer Wound Healing. Stem Cells Int. 2016;2016:3232859 pubmed publisher
Jiang W, Ye L, Ruge F, Owen S, Martin T, Sun P, et al. YangZheng XiaoJi exerts anti-tumour growth effects by antagonising the effects of HGF and its receptor, cMET, in human lung cancer cells. J Transl Med. 2015;13:280 pubmed publisher
Ito Y, Correll K, Zemans R, Leslie C, Murphy R, Mason R. Influenza induces IL-8 and GM-CSF secretion by human alveolar epithelial cells through HGF/c-Met and TGF-α/EGFR signaling. Am J Physiol Lung Cell Mol Physiol. 2015;308:L1178-88 pubmed publisher
D Alessandro L, Samaga R, Maiwald T, Rho S, Bonefas S, Raue A, et al. Disentangling the Complexity of HGF Signaling by Combining Qualitative and Quantitative Modeling. PLoS Comput Biol. 2015;11:e1004192 pubmed publisher
Saito S, Morishima K, Ui T, Hoshino H, Matsubara D, Ishikawa S, et al. The role of HGF/MET and FGF/FGFR in fibroblast-derived growth stimulation and lapatinib-resistance of esophageal squamous cell carcinoma. BMC Cancer. 2015;15:82 pubmed publisher
Holland W, Chinn D, Lara P, Gandara D, Mack P. Effects of AKT inhibition on HGF-mediated erlotinib resistance in non-small cell lung cancer cell lines. J Cancer Res Clin Oncol. 2015;141:615-26 pubmed publisher
Zhou S, Liu L, Li H, Eilers G, Kuang Y, Shi S, et al. Multipoint targeting of the PI3K/mTOR pathway in mesothelioma. Br J Cancer. 2014;110:2479-88 pubmed publisher
Yen B, Yen M, Hsu P, Liu K, Wang C, Bai C, et al. Multipotent human mesenchymal stromal cells mediate expansion of myeloid-derived suppressor cells via hepatocyte growth factor/c-met and STAT3. Stem Cell Reports. 2013;1:139-51 pubmed publisher
Wu Y, Liu C, Huang M, Lai H, Lee P, Hu R, et al. C1GALT1 enhances proliferation of hepatocellular carcinoma cells via modulating MET glycosylation and dimerization. Cancer Res. 2013;73:5580-90 pubmed publisher
Breindel J, Haskins J, Cowell E, Zhao M, Nguyen D, Stern D. EGF receptor activates MET through MAPK to enhance non-small cell lung carcinoma invasion and brain metastasis. Cancer Res. 2013;73:5053-65 pubmed publisher
Grugan K, Vega M, Wong G, Diehl J, Bass A, Wong K, et al. A common p53 mutation (R175H) activates c-Met receptor tyrosine kinase to enhance tumor cell invasion. Cancer Biol Ther. 2013;14:853-9 pubmed publisher
Katayama R, Aoyama A, Yamori T, Qi J, Oh hara T, Song Y, et al. Cytotoxic activity of tivantinib (ARQ 197) is not due solely to c-MET inhibition. Cancer Res. 2013;73:3087-96 pubmed publisher
Accornero P, Miretti S, Bersani F, Quaglino E, Martignani E, Baratta M. Met receptor acts uniquely for survival and morphogenesis of EGFR-dependent normal mammary epithelial and cancer cells. PLoS ONE. 2012;7:e44982 pubmed publisher
Muller F, Colla S, Aquilanti E, Manzo V, Genovese G, Lee J, et al. Passenger deletions generate therapeutic vulnerabilities in cancer. Nature. 2012;488:337-42 pubmed publisher
Goodnough J, Ramos E, Nemeth E, Ganz T. Inhibition of hepcidin transcription by growth factors. Hepatology. 2012;56:291-9 pubmed publisher
Jiao Y, Ou W, Meng F, Zhou H, Wang A. Targeting HSP90 in ovarian cancers with multiple receptor tyrosine kinase coactivation. Mol Cancer. 2011;10:125 pubmed publisher
Tanizaki J, Okamoto I, Sakai K, Nakagawa K. Differential roles of trans-phosphorylated EGFR, HER2, HER3, and RET as heterodimerisation partners of MET in lung cancer with MET amplification. Br J Cancer. 2011;105:807-13 pubmed publisher
Yang X, Turke A, Qi J, Song Y, Rexer B, Miller T, et al. Using tandem mass spectrometry in targeted mode to identify activators of class IA PI3K in cancer. Cancer Res. 2011;71:5965-75 pubmed publisher
Okamoto W, Okamoto I, Arao T, Yanagihara K, Nishio K, Nakagawa K. Differential roles of STAT3 depending on the mechanism of STAT3 activation in gastric cancer cells. Br J Cancer. 2011;105:407-12 pubmed publisher
De Bacco F, Luraghi P, Medico E, Reato G, Girolami F, Perera T, et al. Induction of MET by ionizing radiation and its role in radioresistance and invasive growth of cancer. J Natl Cancer Inst. 2011;103:645-61 pubmed publisher
Qi J, MCTIGUE M, Rogers A, Lifshits E, Christensen J, Jänne P, et al. Multiple mutations and bypass mechanisms can contribute to development of acquired resistance to MET inhibitors. Cancer Res. 2011;71:1081-91 pubmed publisher
Ou W, Hubert C, Corson J, Bueno R, Flynn D, Sugarbaker D, et al. Targeted inhibition of multiple receptor tyrosine kinases in mesothelioma. Neoplasia. 2011;13:12-22 pubmed
Kongkham P, Onvani S, Smith C, Rutka J. Inhibition of the MET Receptor Tyrosine Kinase as a Novel Therapeutic Strategy in Medulloblastoma. Transl Oncol. 2010;3:336-43 pubmed
Qin S, Taglienti M, Nauli S, Contrino L, Takakura A, Zhou J, et al. Failure to ubiquitinate c-Met leads to hyperactivation of mTOR signaling in a mouse model of autosomal dominant polycystic kidney disease. J Clin Invest. 2010;120:3617-28 pubmed publisher
Hoot K, Oka M, Han G, Bottinger E, Zhang Q, Wang X. HGF upregulation contributes to angiogenesis in mice with keratinocyte-specific Smad2 deletion. J Clin Invest. 2010;120:3606-16 pubmed publisher
Cepero V, Sierra J, Corso S, Ghiso E, Casorzo L, Perera T, et al. MET and KRAS gene amplification mediates acquired resistance to MET tyrosine kinase inhibitors. Cancer Res. 2010;70:7580-90 pubmed publisher
Costa B, Dettori D, Lorenzato A, Bardella C, Coltella N, Martino C, et al. Fumarase tumor suppressor gene and MET oncogene cooperate in upholding transformation and tumorigenesis. FASEB J. 2010;24:2680-8 pubmed publisher
Blanco R, Iwakawa R, Tang M, Kohno T, Angulo B, Pio R, et al. A gene-alteration profile of human lung cancer cell lines. Hum Mutat. 2009;30:1199-206 pubmed publisher
Kawaguchi K, Murakami H, Taniguchi T, Fujii M, Kawata S, Fukui T, et al. Combined inhibition of MET and EGFR suppresses proliferation of malignant mesothelioma cells. Carcinogenesis. 2009;30:1097-105 pubmed publisher
Holliday D, Brouilette K, Markert A, Gordon L, Jones J. Novel multicellular organotypic models of normal and malignant breast: tools for dissecting the role of the microenvironment in breast cancer progression. Breast Cancer Res. 2009;11:R3 pubmed publisher
Sierra J, Corso S, Caione L, Cepero V, Conrotto P, Cignetti A, et al. Tumor angiogenesis and progression are enhanced by Sema4D produced by tumor-associated macrophages. J Exp Med. 2008;205:1673-85 pubmed publisher
image
image 1 :
Tocris Bioscience 2693/10 image 1
Cat.No. 2693 - PHA 665752 C32H34Cl2N4O4S CAS No. 477575-56-7
product information
brand :
Tocris
MasterCode :
2693
SKU :
2693/10
product name :
PHA 665752
target :
MET Inhibitors
category :
Small Molecules
unit size :
10 mg (also 50 mg)
purity :
98%
observed molecular weight :
641.61
url print :
?utm_source=biocompare&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
PHA 665752 is a potent, selective and ATP-competitive inhibitor of MET kinase (IC50 values are 9, 68, 200, 1400, 3000, 3800 and 6000 nM for MET, Ron, Flk-1, c-abl, FGFR1, EGFR and c-src respectively and 10000 nM for IGF-IR, PDGFR, AURORA2, PKA, PKB , p38 , MK2 and MK3). Antitumor agent; inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts.
extended description :
Potent and selective MET inhibitor
chemical name text :
(2R)-1-[[5-[(Z)-[5-[[(2,6-Dichlorophenyl)methyl]sulfonyl]-1,2-dihydro-2-oxo-3H-indol-3-ylidene]methyl]-2,4-dimethyl-1H-pyrrol-3-yl]carbonyl]-2-(1-pyrrolidinylmethyl)pyrrolidine
formula :
C 32 H 34 Cl 2 N 4 O 4 S
formula text :
C32H34Cl2N4O4S
cas num :
477575-56-7
USD :
416 USD
product details :
Potent and selective MET inhibitor
storage :
Store at +4°C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK