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. Author manuscript; available in PMC: 2012 Oct 27.
Published in final edited form as: J Med Chem. 2011 Sep 22;54(20):7150–7164. doi: 10.1021/jm200739e

Figure 8. In vivo efficacy trial with compounds 3 and 4 with IGROV1 xenografts.

Figure 8

Human IGROV1 tumors were implanted bilaterally into female ICR SCID mice maintained on a folate-deficient diet and mice were non-selectively randomized into 4–7 mice/group. Compounds 3 (40 mg/mg) and 4 (180 mg/kg and 112.5 mg/kg) [dissolved in 5% ethanol (v/v), 1% Tween-80 (v/v), 0.5% NaHCO3] were administered on a Q4dx5 schedule intravenously (0.2 ml/injection) on days 3, 7, 11, 15, and 19. Mice were observed and weighed daily; tumors were measured twice per week. For the experiment shown, antitumor activity was significant for compound 3 (14% T/C, 2.7 gross log kill) and exceeded that for compound 4 at either dose (32% and 44% T/C, 2.3 and 1.2 gross log kill, respectively at 180 mg/kg and 112.5 mg/kg, respectively). The results are summarized in Table 1S in the Supplement.