Fig. 2: Gimatecan exhibits superior antitumor effect than irinotecan in vitro and in vivo. | Cell Death & Disease

Fig. 2: Gimatecan exhibits superior antitumor effect than irinotecan in vitro and in vivo.

From: A novel oral camptothecin analog, gimatecan, exhibits superior antitumor efficacy than irinotecan toward esophageal squamous cell carcinoma in vitro and in vivo

Fig. 2

a, b Eca-109, KYSE-450, KYSE-140, KYSE-510, TE1, TE10 cells were seeded in 96-well plates overnight in complete medium and then exposed to a gradient dilution of gimatecan (0–125 nM) or irinotecan (0–125 μM) for 48 h. Cell viability was measured, and is presented as the mean ± SD of six replicate assays. c The IC50 values of gimatecan and irinotecan for each cell lines were calculated. Data are presented as the mean ± SD of three replicate assays. d–g In vivo antitumor activity of gimatecan and irinotecan in xenograft models of ESCC cell lines and patient-derived xenograft (PDX) models. Eca-109/KYSE-450 cell lines or PDX tumor tissues were subcutaneously engrafted and grown in NOD/SCID mice until 150–200 mm3. Then the mice were treated with saline containing 10% DMSO, gimatecan (0.25 mg/kg, d1–d5/week, oral gavage), or irinotecan (8 mg/kg, twice a week, i.p.) for 3 weeks, and tumor volume and the body weight of each mouse were measured twice a week. Tumor volume is expressed as the mean ± SD of at least five mice in each group. Antitumor activity was analyzed using an unpaired two-tailed t-test and is depicted by tumor growth inhibition. *P < 0.05, **P < 0.01, ***P < 0.001

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