1. PET determination of specific uptake of 11C-erlotinib by different tumor types expressing EGFR, in vivo, through kinetic modeling
J. Ryan Petrulli1,4, Jenna M. Sullivan1,4, Ming-Qiang Zheng2,4, Yiyun Huang2,4, Joseph N. Contessa3, Evan D. Morris1,2,4
1. Biomedical Engineering
2. Diagnostic Radiology
3. Therapeutic Radiology
4. Yale PET Center
Yale University, New Haven, CT, USA

2. METHODS Subjects: nude mice implanted with 2-3 tumor xenografts
Human cancer cell lines: SW620, U87, HCC827, PC9, and U87∆
Scans: Siemens Focus 220; 11C-erlotinib injections with or without excess erlotinib
Analysis:
Regions of interest (ROI) drawn on summed images; regional time-activity curves
Kinetic modeling with SRTM to produce BP
Statistical comparison between BP in each xenograft and drug condition
U87, U87D = glioblastoma
HCC827, PC9
Kinase Domain
Active
U87∆
Extracellular Domain
U87
WT EGFR
Inactive
Cell Line:
Mutation:
Status:
SW620
No EGFR
n/a

3. KINASE DOMAIN MUTANT TUMORS
Tracer Experiment
Excess Cold Drug
KD Mutant
KD Mutant
no EGFR
SW620 (▲)
Muscle (○)
HCC827 (■)
PC9 (♦)
HCC827, PC9
KD Mutant
Activated EGFR

4. SPECIFIC BINDING ** * NS NS NS ** p<0.05 * p=0.06 Mutation: KD
Active KD
Active
ECD
WT EGFR
Inactive
No EGFR
n/a
Status:
** p< * p=0.06