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Tubulin inhibitor 25
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Tubulin inhibitor 25
CAS No. : 2411697-71-5
MCE 站:Tubulin inhibitor 25
产品活性:Tubulin inhibitor 25 是一种有效的微管蛋白 (tubulin) 抑制剂,IC50 为 0.98 μM。Tubulin inhibitor 25 对 HT29 细胞有显著的抑制作用。Tubulin inhibitor 25 能抑制细胞迁移和微管形成,有助于抗血管生成。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton
作用靶点:Microtubule/Tubulin
In Vitro: Tubulin inhibitor 25 (compound 6c) (0-100 μM; 48 hours) exhibits high antiproliferative activity against tested cancer cell lines.
Tubulin inhibitor 25 (0-200 μM; 48 hours) exhibits low cytotoxicity in normal cell lines.
Tubulin inhibitor 25 (0.05, 0.1 and 0.2 μM; 24 hours) inhibits the colony formation of HT29 cells in a dose-dependent manner.
Tubulin inhibitor 25 (2 and 4 μM) can inhibit the tubulin polymerization and compete with colchicine binding site.
Tubulin inhibitor 25 (0.25-1 μM; 12-48 hours) arrests the cell cycle at G2/M phase and induces HT29 cells apoptosis in a dose- and time-dependent manner, besides induces HT29 cell depolarized mitochondria in the process of apoptosis.
Tubulin inhibitor 25 (0.25-1 μM; 24 hours) increases the expression of P21 and Cyclin B1 and decreases the expression of Cdc2, p-CDC2 and p-Cdc25c; as well as induces the microtubule collapse in HT29 cells in a dose-dependent manner.
Tubulin inhibitor 25 (0.01, 0.02 and 0.04 μM; 6 hours) effectively inhibits the HUVEC tube formation in a dose-dependent manner.
Tubulin inhibitor 25 (0.1, 0.2 and 0.4 μM; 24 hours) inhibits migration of A549 cells in a dose-dependent manner.
In Vivo: Tubulin inhibitor 25 (1.5 mg/kg; IV; single) exhibits good metabolic stability.
Pharmacokinetic Parameters of Tubulin inhibitor 25 in male Sprague-Dawley rats.
IV (1.5 mg/kg) | |
T1/2 (h) | 3.81 ± 2.14 |
MRT0-∞ (h) | 5.12 ± 2.86 |
AUC0-∞ (ng/mLh) | 2156.12 ± 851.88 |
VZ (L/kg) | 3.348 ± 0.734 |
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