KL-11743 是葡萄糖竞争性 I 类葡萄糖转运蛋白抑制剂,口服有活性,能够抑制GLUT1 (IC50:115 nM) 、GLUT2 (IC50:137 nM) 、GLUT3 (IC50:90 nM) 及GLUT4 (IC50:68 nM) 。它能够特异性阻断葡萄糖代谢,也可与电子传递抑制剂协同作用诱导细胞死亡。
产品描述
KL-11743 specifically blocks glucose metabolism, triggering an acute collapse in NADH pools and a striking accumulation of aspartate, indicating a dramatic shift toward oxidative phosphorylation in the mitochondria.
体外活性
Patient-derived xenograft models of succinate dehydrogenase A (SDHA)-deficient cancers are specifically sensitive to KL-11743, providing direct evidence that TCA cycle-mutant tumors are vulnerable to GLUT inhibitors in vivo[1].
Cas No.
1369452-53-8
分子式
C30H30N6O3
分子量
522.609
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years