FX-11

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

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) inhibitor, with a Ki of 8 μM. 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.

Western Blot Analysis Cell Line:P493 cellsConcentration: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 Assay Cell 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 IC50 values of 49.27 μM and 60.54 μM for BxPc-3 and MIA PaCa-2 cells, respectively.

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 daysResult: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.

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Metabolic Enzyme/Protease

Dehydrogenase

Dehydrogenase

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213971-34-7

350.41

C22H22O4

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 250 mg/mL (713.45 mM; 超声助溶 )

CCCc1c(O)c(O)c(C(O)=O)c2cc(Cc3ccccc3)c(C)cc12

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(-20℃)

With Ice Pack

≥ 2 years