Antitumor agent-77 具有抗肿瘤活性，能抑制癌细胞的生长和迁移。Antitumor agent-77 通过抑制 GPx-4 和升高 COX2 引发铁下垂 (ferroptosis)。Antitumor agent-77 还能激活肿瘤细胞固有凋亡通路 (Bax-Bcl-2-caspase-3)，阻碍肿瘤细胞上皮间质转化 (EMT) 过程。
| 生物活性 | Antitumor agent-77 is an antitumor agent, inhibitscancercells growth and migration. Antitumor agent-77 triggersferroptosisby inhibiting GPx-4 and elevating COX2. Antitumor agent-77 also activates intrinsic apoptotic pathway (Bax-Bcl-2-caspase-3) and hinders Epithelial-mesenchymal transition (EMT) process ofcancercells[1]. |
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体外研究
(In Vitro) | Antitumor agent-77 (compound 2a) (30 μM; 4 h) exhibits better solubility and improved cellular uptake thanCarboplatin(HY-17393) in A549 cells[1].
Antitumor agent-77 (20 μM; 36 h) produces cytotoxicity by inducing apoptosis of A549 cancer cells[1].
Antitumor agent-77 (20 μM; 24 h) results in significant down-regulation of Bcl-2 and upregulation of Bax, also leads to E-cadherin increase, Vimentin decrease[1].
Antitumor agent-77 (20 μM; 24 h) arrests cell cycle at S phase and G2/M phase[1].
Antitumor agent-77 (10 μM; 12 h) inhibits cells migration with inhibition rate of 52%[1].
Apoptosis Analysis[1] | Cell Line: | A549 cells | | Concentration: | 20 μM | | Incubation Time: | 36 hours | | Result: | Resulte cell apopsotsis with average apoptotic values (including both early and late apoptotic states which were displayed in Q1-LR and Q1-UR, respectively) of 25.34%. |
Western Blot Analysis[1] | Cell Line: | A549 cells | | Concentration: | 20 μM | | Incubation Time: | 24 hours | | Result: | Elevated the level of cleaved caspase-3 and reduced the level of caspase-3 in A549 cells.
Decreased anti-apoptotic protein Bcl-2 and increased pro-apoptotic protein Bax.
Elevated the expression of E-cadherin and on the other hand, lowered the protein level of Vimentin. |
Cell Cycle Analysis[1] | Cell Line: | A549 cells | | Concentration: | 20 μM | | Incubation Time: | 24 hours | | Result: | Blocked cell cycle progression in S and G2/M phase with the values of 41.11% and 26.03%, respectively. |
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体内研究
(In Vivo) | Antitumor agent-77 (compound 2a) (6 μg/kg; i.v.; injected on day 8, 10, 12) exhibits similar potency compared withOxaliplatin(HY-17371), without significant damage to kidney and liver as well as weight loss[1].
| Animal Model: | A549 xenograft models in mouse[1] | | Dosage: | 6 μg/kg | | Administration: | Intravenous injection; administration on day 8, 10, 12 after establishing xenograft models (A549 cells; s.c.) | | Result: | Significantly repressed tumor growth, and maintained normal kidney and liver architecture in mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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