1. Volume 5, Issue 3, Pages 231-239 (March 2004)
In vivo antitumor activity of NVP-AEW541—A novel, potent, and selective inhibitor of the IGF-IR kinase 
Carlos Garcı́a-Echeverrı́a, Mark A Pearson, Andreas Marti, Thomas Meyer, Juergen Mestan, Johann Zimmermann, Jiaping Gao, Josef Brueggen, Hans-Georg Capraro, Robert Cozens, Dean B Evans, Doriano Fabbro, Pascal Furet, Diana Graus Porta, Janis Liebetanz, Georg Martiny-Baron, Stephan Ruetz, Francesco Hofmann 
Cancer Cell 
Volume 5, Issue 3, Pages (March 2004)
DOI: /S (04)

2. Figure 1 Inhibition of IGF-IR signaling by NVP-AEW541 in NWT-21 cells
Inhibition of IGF-IR-mediated signaling by NVP-AEW541 was determined in NWT-21 cells, a derivative of NIH3T3 mouse fibroblasts obtained upon overexpression of the human IGF-IR. Cells were grown as a monolayer, exposed to NVP-AEW541, and stimulated with IGF-I. IGF-IR and PKB phosphorylation, as well as their total protein levels, were determined by Western blot as described in the Experimental Procedures.
Cancer Cell 2004 5, DOI: ( /S (04) )

3. Figure 2
Inhibition of IGF-IR signaling by NVP-AEW541 in a mouse pharmacodynamic model
Inhibition of IGF-IR-mediated signaling by NVP-AEW541 in murine lung was determined ex vivo as described in the Experimental Procedures. NVP-AEW541 was administered p.o. at 50 mg/kg; one hour later, IGF-I at 0.1 mg/kg was injected i.v., and the tissue was collected 5 min thereafter. IGF-IR, PKB, and MAPK phosphorylation, as well as their total levels to ensure equal loading, were determined ex vivo by immunoprecipitation-Western blot (phospho-IGF-IR) or by Western blot.
Cancer Cell 2004 5, DOI: ( /S (04) )

4. Figure 3
Inhibition of IGF-IR signaling by NVP-AEW541 in NWT-21 tumor xenografts
Inhibition of IGF-IR-mediated signaling by NVP-AEW541 in subcutaneous NWT-21 tumors was determined ex vivo as described in the Experimental Procedures. NVP-AEW541 was administered p.o. at 50 mg/kg; one hour later, tumor tissue was collected with or without prior stimulation with IGF-I (0.1 mg/kg) by i.v. injection. IGF-IR, PKB, and MAPK phosphorylation, as well as their total levels to ensure equal loading, were determined ex vivo by Western blot.
Cancer Cell 2004 5, DOI: ( /S (04) )

5. Figure 4
Inhibition of tumor growth by oral administration of NVP-AEW541 in a fibrosarcoma model
Tumors were established in female nude mice (Hsd:Athymic Nude-nu) by subcutaneous implantation of NWT-21 tumor fragments (3 × 3 × 3 mm) obtained from donor mice. Seven days after implantation (day 0), treatment with NVP-AEW541 was started at doses of 20 mg/kg, 30 mg/kg, and 50 mg/kg p.o. bid, 7×/week. Vehicle controls received 25 mM L(+)-tartaric acid p.o. bid, 7×/week. Tumor volumes were determined according to the formula L × W × H × π / 6 and are shown in mm3 as mean ± SEM. Body weights are shown in g as mean ± SEM. The experiment was terminated 11 days after start of treatment. *p < 0.05 (Dunnett's) versus control vehicle.
Cancer Cell 2004 5, DOI: ( /S (04) )