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) 特异性抑制剂，Ki为 8 μM。FX-11 可有效激活PKM2(丙酮酸激酶 M2)。FX-11 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。
| 生物活性 | FX-11 is a potent, selective, reversible and competitivelactate dehydrogenaseA(LDHA) specific inhibitor, with aKiof 8 μM. FX-11 can effectively activatePKM2(pyruvate kinase M2). FX-11 reduces ATP levels and induces oxidative stress,ROSproduction and cell death. FX-11 showsantitumoractivity in lymphoma and pancreaticcancerxenografts[1][2]. |
| IC50& Target | IC50: 23.3 μM (LDHA in HeLa cell)[1]. |
体外研究
(In Vitro) | FX-11 (9 μM, 24-48 h) shows activation of AMP kinase and phosphorylation of its substrate acetyl-CoA carboxylase[2].
FX-11 (0-100 μM, 72 h) inhibits cell proliferation in BxPc-3 and MIA PaCa-2 cells[3].
FX-11 inhibits glycolysis and alters cellular energy metabolism in P493 cells[2].
Western Blot Analysis[2] | Cell 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 Assay[3] | 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 IC50values of 49.27 μM and 60.54 μM for BxPc-3 and MIA PaCa-2 cells, respectively. |
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体内研究
(In Vivo) | FX-11 (42 μg/mouse; IP, daily for 10-14 days) inhibits P493 tumor growth[2].
FX-11 (0-2 mg/kg, IP, daily, for 3 weeks) significantly delays tumor growth[3].
| Animal Model: | Male SCID mice and RH-Foxn1nu mice (human P493 B-cell xenografts)[2] | | 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)[3] | | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 250 mg/mL(713.45 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8538 mL | 14.2690 mL | 28.5380 mL | | 5 mM | 0.5708 mL | 2.8538 mL | 5.7076 mL | | 10 mM | 0.2854 mL | 1.4269 mL | 2.8538 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.94 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.94 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.94 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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