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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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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