Aurothiomalate sodium 是一种有效的和选择性的致癌PKCι信号传导抑制剂。Aurothiomalate sodium 抑制肿瘤细胞增殖，而不抑制细胞凋亡。Aurothiomalate sodium 是一种有效的硫氧还蛋白还原酶 (TrxR) 抑制剂。Aurothiomalate sodium 是一种抗风湿剂，显示出有效的抗肿瘤活性。
| 生物活性 | Aurothiomalate sodium is a potent and selective oncogenicPKCιsignaling inhibitor. Aurothiomalate sodium inhibits tumor cell proliferation and not cellapoptosis. Aurothiomalate sodium is a potentthioredoxin reductase (TrxR)inhibitor. Aurothiomalate sodium, an anti-rheumatoid agent, exhibits potent anti-tumor activity[1][2][3]. |
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体外研究
(In Vitro) | Aurothiomalate sodium (0.001, 0.01, 0.1, 1, 10, 100, 1000 uM) induces dose-dependent inhibition of anchorage-independent growth in all cell lines tested (A549, H1437, H2170, H460, H510, H187, H1703 and A427 lung cancer cell lines) with IC50s ranging from 300 nM-107 μM. The lung adenocarcinoma (LAC) and small cell lung carcinoma (SCLC) cells tends to be more sensitive and lung adenocarcinomas (LACs) less sensitive to Aurothiomalate sodium[1].
Aurothiomalate sodium (25 uM; 6 hours) suppresses TNFa-induced activation of NF-kB and the expression of NF-kB-targeted proinflammatory genes such as E-selectin and cyclooxygenase-2[3].
Aurothiomalate sodium inhibits non-small lung cancer (NSCLC) growth by binding PKCιand blocking activation of a PKCι-Par6-Rac1-Pak-Mek 1,2-Erk 1,2 signaling pathway[1].
Aurothiomalate sodium inhibits Mek/Erk signaling and decreases proliferative index without effecting tumor apoptosis or vascularization in vivo[1].
Western Blot Analysis[1] | Cell Line: | Bovine arterial endothelial cells (BAEC) | | Concentration: | 25 uM | | Incubation Time: | 6 hours | | Result: | Suppressed TNFa-induced NF-kB-dependent gene expression in a dose-dependent manner.
Did not affect TrxR1 mRNA level in COS7 cells. |
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体内研究
(In Vivo) | Aurothiomalate sodium (2, 6, 20 or 60 mg/kg/day; intramuscular injections; 40 days) exhibits statistically significant inhibition of tumor growth at all concentrations tested in A427 cell tumors because A427 cells are highly responsive[1].
Aurothiomalate sodium (20, 60 mg/kg/day; intramuscular injections; 15 days) shows a statistically significant response (~50% reduction in tumor size) only at the 60 mg/kg dose in H460 tumors because H460 cells are less responsive[1].
Aurothiomalate sodium (60 mg/kg/day; IP; for six weeks) exhibites a decrease in tumor growth in Three-week-old KrasLA2 mice. Aurothiomalate sodium inhibits Kras-mediated bronchioalveolar stem cells (BASCs) expansion and lung tumorigenesis in vivo[2].
| Animal Model: | 4-6-week-old female nude mice with A427 or H460 cells[1] | | Dosage: | 2, 6, 20 or 60 mg/kg | | Administration: | Intramuscular injections; daily; 40 days | | Result: | Exhibited statistically significant inhibition of tumor growth at all concentrations tested in A427 cell tumors because A427 cells are highly responsive. |
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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 : 250 mg/mL(Need ultrasonic) 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： PBS Solubility: 50 mg/mL (Infinity mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
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