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KL-11743

CAS No. : 1369452-53-8

MCE 站：KL-11743

产品活性：KL-11743 是一种有效的，具有口服活性的葡萄糖竞争性 I 类葡萄糖转运蛋白抑制剂，抑制 GLUT1，GLUT2，GLUT3 和 GLUT4 的 IC₅₀ 值分别为 115 nM，137 nM，90 nM 和 68 nM。KL-11743 特异性阻断葡萄糖代谢。KL-11743 可与电子传递抑制剂协同诱导细胞死亡。

研究领域：Membrane Transporter/Ion Channel

作用靶点：GLUT

In Vitro: KL-11743 (compound 8) competes with glucose for binding to GLUT1, with IC₅₀s of 33 nM ａnd 268 nM at 0.37 mM ａnd 10 mM glucose, respectively.
KL-11743 (39-10000 nM; 24-72 h) dose-dependently inhibits the growth of HT-1080 cells, with an IC₅₀ of 677 nM.
KL-11743 inhibits the growth of KEAP1-mutant lung cancer cells with more potency compared to KEAP1-WT lung cancer cells.
KL-11743 (0.001-10 μM) induces a rapid increase in the phosphorylation of AMPK ａnd acetyl-coenzyme A carboxylase in HT-1080 cells .
KL-11743 (2 μM) inhibits glucose uptake in 786-O cells. KL-11743 increases NADP+/NADPH in NCl-H226 cells. KL-11743 induces cell death in SLC7A11-high cancer cell lines (NCl-H226 ａnd UMRC6 cells).
KL-11743 (0.001-10 μM) inhibits both glucose consumption, lactate secretion, ａnd 2DG transport in HT-1080 fibrosarcoma cells, with IC₅₀s of 228, 234, ａnd 87 nM, respectively, ａnd fully inhibited glycolytic ATP production in oligomycin-treated cells with an IC₅₀ of 127 nM.

In Vivo: KL-11743 (100 mg/kg; i.p. every two days for 5 weeks) decreases the growth of SLC7A11-high NCI-H226 xenograft tumors ａnd was well-tolerated in vivo.
KL-11743 (30-100 mg/kg; a single p.o.) significantly elevates blood glucose levels ａnd delays glucose clearance in mice challenged with 5 g/kg glucose.
KL-11743 significantly suppresses the growth of KEAP1 KO tumors.
Plasma levels of KL-11743 (100 mg/kg; i.p.) are maintained at inhibitory levels for most of the 24-hour dosing period.
KL-11743 (p.o) exhibits moderate oral between 30% ａnd 15%, ａnd favorable ａnd dose-linear plasma exposure profile reaching concentrations of approximately 20 μM in mice (10-100 mg/kg) ａnd rats (10-300 mg/kg).
KL-11743 exhibits comparable half-lives ranging between 2.04 ａnd 5.38 h in rats (10 mg/kg for i.v.; 10-300 mg/kg for p.o.), ａnd 1.45-4.75 h in mice (10 mg/kg for i.v. ａnd i.p.; 10-100 mg/kg for p.o.).

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