货号	规格	价格	上海	北京	珠海	重庆	武汉
S89467-5mg	≥98%	￥1500.00 S89467-5mg ￥1500.00 3-5天	0 货期：3-5天	-	-	-	-
S89467-10mg	≥98%	￥2400.00 S89467-10mg ￥2400.00 3-5天	0 货期：3-5天	-	-	-	-
S89467-25mg	≥98%	￥4500.00 S89467-25mg ￥4500.00 3-5天	0 货期：3-5天	-	-	-	-
S89467-100mg	≥98%	￥13500.00 S89467-100mg ￥13500.00 3-5天	0 货期：3-5天	-	-	-	-

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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

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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