Figure 5. Expression of EphA2 and cellular and in vivo activity of drug conjugates.
(A) Groups of 5–7 SCID-beige mice bearing pre-established subcutaneous PC3 tumors were treated with twice weekly with intravenous doses of vehicle (CT), paclitaxel (5 mg/Kg), YSA-taxol (equimolar doses of the taxol dose), starting at day 0. Tumor sizes were measured and averages ± SEM are shown. p<0.05 for the comparison of YSA-taxol with control, by repeated-measures two-way ANOVA using all the measurements as well as by one-way ANOVA and Dunnett's posthoc test using the measurements at day 18. (B) Bio-distribution analysis. PC3 tumors (n = 3; average volume 200 mm ) were excised 30 min after equimolar amounts of YSA-PTX or PTX (25 mg/kg) were injected intravenously. LC/MS analysis was performed to quantify PTX levels from tumor extracts. The histogram shows averages ± SEM. p<0.05 for the comparison of PTX levels, by t-test analysis. Plasma levels of PTX were not significantly different (YSA-PTX = 998 ± 742 ng/mL; PTX = 771 ± 585 ng/mL).