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说明
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。
Information
DRB18 DRB18 is a pan-GLUT (glucose transporters) inhibitor that inhibits growth and proliferation in several different cancer types with IC50 high nM range.
Targets
GLUT
In vitro
DRB18 inhibits growth and proliferation in about 90% of the 60 different cancer cell lines in 9 major cancer types. DRB18 treatment leads to significant changes in glucose-based metabolism in A549 lung cancer cells, including cell death via ER/oxidative stress and necrosis.
In vivo
DRB18 (10 mg/kg) treatment thrice a week significantly reduces growth in Xenograft A549 tumors.