DRB18

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 细胞中的能量相关代谢。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。DRB18 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. DRB18 has anti-tumor activity.

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 AnalysisCell 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.

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.

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Others

Other Targets

transporter

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2863686-81-9

382.88

C22H23ClN2O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 50 mg/mL (130.59 mM; 超声助溶 (<60°C)

CC1=C(C=C(C=C1)CNC2=C(C=C(C=C2)Cl)NCC3=CC(=C(C=C3)C)O)O

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(-20℃)

With Ice Pack

≥ 2 years