Article Images
Content deleted Content added
m |
|||
Line 32: '''AEE788'''<ref>[http://www.selleckchem.com/products/AEE788.html Biological Activity of AEE788]</ref> is a novel multitargeted [[HER2/neu|human epidermal receptor]] (HER) 1/2 and [[vascular endothelial growth factor receptor]] (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC<sub>50</sub> of 2, 6, 77, 59 nM for [[Epidermal growth factor receptor|EGFR]], [[ErbB2]], [[Kinase insert domain receptor|KDR]], and [[Flt-1]].<ref name="pmid15256466">{{cite journal | author = Traxler P, Allegrini PR, Brandt R, Brueggen J, Cozens R, Fabbro D, Grosios K, Lane HA, McSheehy P, Mestan J, Meyer T, Tang C, Wartmann M, Wood J, Caravatti G. | title = AEE788: a dual family epidermal growth factor receptor/ErbB2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity | journal = Cancer Res. | volume = 64 | issue = 14 | pages = 4931–41 | year = 2004 | month = Jul | pmid = 15256466 }}</ref> In cells, growth factor-induced EGFR and ErbB2 phosphorylation was also efficiently inhibited with IC<sub>50</sub>s of 11 and 220 nM, respectively. It efficiently inhibited growth factor-induced EGFR and ErbB2 phosphorylation in tumors for >72 h, a phenomenon correlating with the antitumor efficacy of intermittent treatment schedules. It also inhibits VEGF-induced angiogenesis in a murine implant model. It has potential as an anticancer agent targeting deregulated tumor cell proliferation as well as angiogenic parameters.<ref name="pmid19473483">{{cite journal | author = Juengel E, Engler J, Natsheh I, Jones J, Mickuckyte A, Hudak L, Jonas D, Blaheta RA. | title = Combining the receptor tyrosine kinase inhibitor AEE788 and the mammalian target of rapamycin (mTOR) inhibitor RAD001 strongly inhibits adhesion and growth of renal cell carcinoma cells | journal = BMC Cancer. | volume = 9 | issue = 161| year = 2009 | month = May | pmid = 19473483 }}</ref><ref name="pmid20885895">{{cite journal | author = Meco D, Servidei T, Zannoni GF, Martinelli E, Prisco MG, de Waure C, Riccardi R. | title = Dual Inhibitor AEE788 Reduces Tumor Growth in Preclinical Models of Medulloblastoma. | journal = Transl Oncol. | volume = 3 | issue = 5| pages = 326–35 | year = 2010 | month = Oct| pmid = 20885895 }}</ref><br />
{| class="wikitable" |- Line 39: | EGFR ICD || 2 |- | [[http://en.wikipedia.org/wiki/ErbB2|ErbB2]] (HER-2) || 6 |- | [[ErbB4]] (HER-4) || 160 |- | [[KDR]] || 77 |- | Tek || 2100 Line 51: | Ins-R || >10000 |- | [[PDGFR]]-beta || 320 |- | c-Met || 2900 Line 73: | Cdk1/Cyc.B || 8000 |- | [[PKC-alpha]] || >10000 |- | c-Raf-1 || 2800 |- | [[PKA]] || >10000 |}<br />
{| class="wikitable" |- Line 96: | 32D/EGFRvIII || 10 |- | [[MCF-7]] || 2500 |- | MCF-7/EGFRvIII || <5000 | |||