FX-11

FX-11 是一种有效的、选择性的、可逆的和竞争性的乳酸脱氢酶 A (LDHA) 抑制剂，Ki 为 8 μM。FX-11 可降低 ATP 水平，诱导氧化应激、ROS 生成和细胞死亡。FX-11 在淋巴瘤和胰腺癌异种移植中显示出抗肿瘤 (antitumor) 活性。 FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A ( LDHA ) specific inhibitor, with a K i of 8 μM. FX-11 can effectively activate PKM2 (pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts In Vitro FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase. ? FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells. ? FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: P493 cells Concentration: 9 μM Incubation Time: 24 h, 48 h Result: Showed a decrease in ATP levels, accompanied by activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase. Cell Proliferation AssayCell Line: BxPc-3 and MIA PaCa-2 cells Concentration: 0-100 µM Incubation Time: 72 h Result: Reduced cell metabolic activity in a concentration-dependent manner, showed a significant reduction in cell proliferation, with IC 50 values of 49.27 µM and 60.54 µM for BxPc-3 and MIA PaCa-2 cells, respectively. In Vivo FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth. ? FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)Dosage: 42 µg/mouse (2.1 mg/kg) Administration: IP; daily for 10-14 days Result: Resulted in a remarkable inhibition of tumor growth, inhibited tumor xenograft progression. Animal Model: Immunocompromised CD-1 mice (6-8 weeks; 20-25 g, n=5 per group)Dosage: 2 mg/kg, 1 mg/kg+15 mg/kg TEPP-46, 2 mg/kg+30 mg/kg TEPP-46 Administration: IP (100 µL), daily, for 3 weeks Result: Significantly lowered LDHA activity in plasma and tumor lysates; significantly lowered the expression of the proliferation marker Ki-67; significantly decreased proliferation indices were observed in tumor sections; significantly delayed tumor growth. Form:Solid IC50& Target:IC50: 23.3 μM (LDHA in HeLa cell)

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