Figure 4
From: Hetero-modification of TRAIL trimer for improved drug delivery and in vivo antitumor activities
Biological activities of PEG-TRAIL-vcMMAE
(a) Selective induction of G2 growth arrest. MCF-7 cells were exposed to 1 μM N109C and its conjugates or 0.5 μM MMAE for 8 hrs before analysis by flow cytometry. Blue peak designates the position of G2-M phase populations. %G2/M indicates the percentage of cells arrested at the G2-M phase. (b) Pharmacokinetic profiles of N109C and its conjugates. Sprague-Dawley (SD) rats were administered an i.v. injection of N109C, N109C-vcMMAE or PEG-N109C-vcMMAE (1 mg per rat) and their concentrations in blood were determined by ELISA. Results are expressed as mean ± S.D. from 4 different rats (n = 4). (c) In vivo distribution of PEG-N109C-Cy5. Tumor locations were designated by white arrows. Both flanks of PEG-N109C-Cy5 group mouse were inoculated with NCI-H460 cells.
