• 产品描述： DRB18 is a potent pan-class GLUT inhibitor. DRB18 alters energy-related metabolism in A549 cells by changing the abundance of metabolites in glucose-related pathways. DRB18 can eventually lead to G1/S phase arrest and increase oxidative stress and necrotic cell death. DRB18 has anti-tumor activity

• 靶点： GLUT

• 体外研究：
  DRB18 (0-10 μM；30 分钟) 以剂量依赖性方式降低表达 GLUT1-4 的 HEK293 细胞系中的葡萄糖摄取，IC50 范围从 ~ 900 nM 到 ~ 9 μM。 DRB18 (5 和 10 μM；72 小时) 导致 G1/S 期转变中的细胞周期停滞。 DRB18 (5 和 10 μM；72 小时) 增加 A549 细胞中的 ROS 水平。 DRB18 (5 和 10 μM；72 小时) 降低糖基化 GLUT1 和 GLUT2-4 的表达A549细胞呈剂量依赖性。 Cell Proliferation Assay Cell Line: GLUT1-4-expressed HEK293 cell lines Concentration: 0-10 μM Incubation Time: 30 min Result: Reduced glucose uptake in these cell lines in a dose-dependent manner with IC50s varying from ~ 900 nM to ~ 9 μM. Cell Cycle Analysis Cell Line: A549 Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Caused cell cycle arrest in the G1/S phase transition. Western Blot Analysis Cell Line: A549 Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner. Western Blot Analysis Cell Line: A549 Concentration: 5 and 10 μM Incubation Time: 72 hours Result: Reduced expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner.

• 体内研究：
  DRB18 (10 mg/kg；腹腔注射；每周三次，持续 5 周) 可抑制 44% 的肿瘤体积和 43% 的肿瘤重量。 Animal Model: Male NU/J nude mice (3-4 weeks; tumor cell-injected) Dosage: 10 mg/kg Administration: IP; thrice a week for 5 weeks Result: The tumors were 44% smaller by volume and 43% smaller by weight, also showed DRB18 decreased expression of GLUT1-4 (Fig. 5f) and reduced proliferative capacity within the xenografted tumor.

• 参考文献：
  1. Shriwas P, Roberts D, Li Y, et al. A small-molecule pan-class I glucose transporter inhibitor reduces cancer cell proliferation in vitro and tumor growth in vivo by targeting glucose-based metabolism. Cancer Metab. 2021;9(1):14. Published 2021 Mar 26.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.612 ml	13.059 ml	26.118 ml
  5 mM	0.522 ml	2.612 ml	5.224 ml
  10 mM	0.261 ml	1.306 ml	2.612 ml
  50 mM	0.052 ml	0.261 ml	0.522 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *