Tubulin inhibitor 11 是一种有效的具有口服活性的微管蛋白 (tubulin) 抑制剂。Tubulin inhibitor 11 靶向微管蛋白上的秋水仙碱结合位点，抑制微管蛋白聚合，促进有丝分裂阻断和细胞凋亡 (apoptosis)。
| 生物活性 | Tubulin inhibitor 11 is a potent and orally activetubulininhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade andapoptosis[1]. |
体外研究
(In Vitro) | Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis[1].
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50of 8 nM[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner[1].
Cell Cycle Analysis[1] | Cell Line: | DU145 cells | | Concentration: | 0.01 μM, 0.03 μM, and 0.1 μM | | Incubation Time: | 12 hours | | Result: | Caused cell cycle arrest at G2/M phase. |
Apoptosis Analysis[1] | Cell Line: | DU145 cells | | Concentration: | 0.03 μM, 0.1 μM, and 0.3 μM | | Incubation Time: | 48 hours | | Result: | Induced cancer cell apoptosis. |
Western Blot Analysis[1] | Cell Line: | DU145 cells | | Concentration: | 0.01 μM, 0.03 μM, and 0.1 μM | | Incubation Time: | 12 hours | | Result: | Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells. |
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体内研究
(In Vivo) | Tubulin inhibitor 11 (Compound 48; 5-10 mg/kg; p.o; once daily) shows robust in vivo antitumor efficacies[1].
| Animal Model: | Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells[1] | | Dosage: | 5 mg/kg, 10 mg/kg | | Administration: | p.o; once daily | | Result: | Effectively suppressed tumor growth. |
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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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