DRB18 是一种有效的葡萄糖转运蛋白 (GLUT) 泛抑制剂。DRB18 通过改变葡萄糖相关途径中代谢产物的丰度来改变 A549 细胞中能量相关的代谢。DRB18 最终可导致细胞阻滞在 G1/S 期，增加氧化应激和坏死细胞死亡，具有抗肿瘤活性。

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 and has anti-tumor activity [1].

DRB18 (0-10 μM; 30 min) reduces glucose uptake in GLUT1-4-expressed HEK293 cell lines in a dose-dependent manner with IC 50 s varying from ~ 900 nM to ~ 9 μM [1]. DRB18 (5 and 10 μM; 72 hours) results in cell cycle arrest in the G1/S phase transition [1]. DRB18 (5 and 10 μM; 72 hours) increases ROS levels in A549 cells [1]. DRB18 (5 and 10 μM; 72 hours) reduces expression of glycosylated GLUT1 and GLUT2-4 in A549 cells in a dose-dependent manner [1]. Cell Proliferation Assay Cell Line: GLUT1-4-expressed HEK293 cell lines [1] Concentration: 0-10 μM Incubation Time: 30 min Result: Reduced glucose uptake in these cell lines in a dose-dependent manner with IC 50 s varying from ~ 900 nM to ~ 9 μM. Cell Cycle Analysis Cell Line: A549 [1] 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 [1] 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 [1] 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.

DRB18 (10 mg/kg; IP; thrice a week for 5 weeks) significantly inhibits tumors volume by 44% and tumors weight by 43% [1]. Animal Model: Male NU/J nude mice (3-4 weeks; tumor cell-injected) [1] 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.

T22317

C22H23ClN2O2

382.88

DMSO:45 mg/mL (117.5 mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years