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Tubulin Polymerization-IN-1 prodrug (Compound 2b) 是一种通过Pd-介导的微管蛋白聚合抑制剂前药。它基于秋水仙碱结合位点抑制剂 (CBSIs) 设计,通过降低毒性和提升靶向释放性能。相较于母体化合物,Tubulin Polymerization-IN-1 prodrug 的细胞毒性减少了68.3倍,但在存在Pd树脂时,可原位恢复其细胞毒性。机制研究显示,其抗肿瘤活性与CBSIs一致。在体内实验中,经Pd树脂激活后,Tubulin Polymerization-IN-1 prodrug 能明显抑制肿瘤生长(抑制率63.2%)。该化合物在抗癌研究中展现出潜在应用前景。
Tubulin Polymerization-IN-1 prodrug (Compound 2b) 是一种通过Pd-介导的微管蛋白聚合抑制剂前药。它基于秋水仙碱结合位点抑制剂 (CBSIs) 设计,通过降低毒性和提升靶向释放性能。相较于母体化合物,Tubulin Polymerization-IN-1 prodrug 的细胞毒性减少了68.3倍,但在存在Pd树脂时,可原位恢复其细胞毒性。机制研究显示,其抗肿瘤活性与CBSIs一致。在体内实验中,经Pd树脂激活后,Tubulin Polymerization-IN-1 prodrug 能明显抑制肿瘤生长(抑制率63.2%)。该化合物在抗癌研究中展现出潜在应用前景。
产品描述 | Tubulin Polymerization-IN-1 prodrug (Compound 2b) is a microtubule polymerization inhibitor prodrug mediated by Pd. Developed from colchicine-binding site inhibitors (CBSIs), it aims to reduce toxicity and enhance targeted release. Compared to the parent compound, its cytotoxicity is decreased by 68.3 times, but can be in situ restored in the presence of Pd resin. Mechanistic studies show it retains the same antitumor activity as CBSIs. In vivo tests demonstrate that, once activated by Pd resin, it significantly suppresses tumor growth (63.2% inhibition rate). Tubulin Polymerization-IN-1 prodrug is a promising candidate for cancer research. |
分子量 | 398.43 |
分子式 | C22H23FN2O4 |
CAS No. | 3033099-32-7 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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