Oxamic acid (oxamate) sodium salt 是一种LDH-A(乳酸脱氢酶-A) 抑制剂。Oxamic acid sodium salt 表现出抗肿瘤活性,对癌细胞的抗增殖活性,并可诱导细胞凋亡。
生物活性 | Oxamic acid (oxamate) sodium salt is alactate dehydrogenase-A(LDH-A) inhibitor. Oxamic acid sodium salt shows anti-tumor activity, and anti-proliferative activity againstcancercells, and can induceapoptosis[1][2][3]. |
体外研究 (In Vitro) | Oxamic acid suppresses the proliferation, migration and invasion of both A2780 and SKOV3 cells[1]. Oxamic acid (10 μM; 24-72 h) inhibits cell proliferation in a dose- and time-dependent manner in both NPC cancer cells[2]. Oxamic acid (0-100 mM; 24 h) induces cell cycle arrest in the G2/M phase in CNE-1 and CNE-2 cells[2]. Oxamic acid (0-100 mM; 48 h) induces apoptosis via caspase-3 activation and the mitochondrial pathway in NPC cells[2]. Oxamic acid (0-100 mM; 24 h) increases ROS levels in NPC cells[2].
Cell Proliferation Assay[2] Cell Line: | CNE-1 and CNE-2 cells | Concentration: | 10 μM | Incubation Time: | 24-72 hours | Result: | Showed IC50s of 74.6, 32.4 and 17.8 mM and 62.3, 44.5, 31.6 mM at 24, 48 and 72 h in the CNE-1 and CNE-2 cancer cells, respectively. |
Apoptosis Analysis[2] Cell Line: | 0, 20, 50 and 100 mM | Concentration: | 10 μM | Incubation Time: | 48 hours | Result: | Showed the increasement of early and late apoptotic cells in a dose-dependent manner. Increased the expression of pro-apoptotic Bax and cleaved-caspase-3, while reduced the anti-apoptotic signals of Bcl-2 and pro-caspase-3. |
Cell Cycle Analysis[2] Cell Line: | 0, 20, 50 and 100 mM | Concentration: | 10 μM | Incubation Time: | 24 hours | Result: | Showed a dose-dependent increase in the numbers of CNE-1 and CNE-2 cells in the G2/M phase. |
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体内研究 (In Vivo) | Oxamic acid (intraperitoneal injection; 750 mg/kg; once daily; 3 w) treatment improves the efficacy of tumor inhibition in vivo when combined with irradiation treatment[2].
Animal Model: | Female Balb/c nude mice injected with CNE-1 cells[2] | Dosage: | 750 mg/kg | Administration: | Intraperitoneal injection; 750 mg/kg; once daily; 3 weeks | Result: | Inhibited the tumor growth when compared to either oxamate alone or irradiation alone. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: H2O : 25 mg/mL(225.16 mM;ultrasonic and warming and heat to 60℃) DMSO : 3.23 mg/mL(29.09 mM;ultrasonic and warming and adjust pH to 5 with HCl and heat to 60℃) 配制储备液 1 mM | 9.0066 mL | 45.0329 mL | 90.0658 mL | 5 mM | 1.8013 mL | 9.0066 mL | 18.0132 mL | 10 mM | 0.9007 mL | 4.5033 mL | 9.0066 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |