BE-43547 has in vivo anti-tumor activity in mouse tumor models

Tumor volume and body weight:
Tumor volume in mice bearing C3H mammary adenocarcinoma subcutaneous foot tumors, treated with vehicle (DMSO) or 5 mg/kg of BE-43547 for 7 consecutive days (indicated by arrows) starting when tumors reached 200 mm3 (day 1). Mice were sacrificed when the maximum allowable tumor volume was reached or when mice showed clear signs of morbidity, this was the case for two mice in the treated group. Body weight of the same mice can also be found in the Excel-file.

18FDG and HE staining of SiHa tumor slices:
Visual comparison of intratumoral glycolytic activity (18FDG) and necrosis (HE) in representative SiHa tumor slices after treatment with a single IP injection of BE-43547 congeners at 10 mg/kg followed by one resting day, and then one IP injection on each 4 consecutive days at 5 mg/kg.One day after the last treatment, mice were injected IP with the glucose tracer analogue 18FDG. One hour later mice were sacrificed and tumors were removed and snap-frozen in pre-cooled isopentane. Subsequently, multiple 10 µm tumor sections were prepared using a cryostat, and analyzed for intratumoral glucose retention (FDG) with digital autoradiography. Following autoradiographic analysis, tissue sections were hematoxylin and eosin (H&E) stained for visualization of necrosis and digitalized using a Hamamatsu NanoZoomer slide scanner (Hamamatsu Photonics, Shizuoka, Japan).

肿瘤体积与体重：
C3H小鼠皮下足部乳腺腺癌移植瘤的肿瘤体积，经DMSO溶剂（对照组）或BE-43547 5 mg/kg连续治疗7天（箭头所示，自肿瘤体积达到200 mm³的起始日算起）。当肿瘤体积达到最大可接受值或小鼠出现明显的疾病症状时，对小鼠进行安乐死，治疗组中有两只小鼠符合此情况。同一小鼠的体重信息亦可在Excel文件中找到。
SiHa肿瘤切片的18FDG和HE染色：
经BE-43547同系物在10 mg/kg剂量下进行单次腹腔注射治疗后，经过一天的休息期，随后每4天进行一次5 mg/kg的腹腔注射，对代表性SiHa肿瘤切片进行18FDG肿瘤内糖酵解活性（18FDG）和坏死（HE）的视觉比较。最后一次治疗后的第1天，对小鼠进行腹腔注射葡萄糖示踪剂18FDG。1小时后，对小鼠进行安乐死，取出肿瘤并迅速冷冻于预冷的异戊烷中。随后，使用冷冻切片机制备多个10 µm的肿瘤切片，并通过数字放射性自显影分析肿瘤内的葡萄糖滞留（FDG）。在放射性自显影分析之后，组织切片用苏木精和伊红（H&E）染色以可视化坏死，并使用Hamamatsu NanoZoomer切片扫描仪（Hamamatsu Photonics，静冈，日本）进行数字化。