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Tubulin polymerization-IN-6
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Tubulin polymerization-IN-6
MCE 站:Tubulin polymerization-IN-6
产品活性:Tubulin polymerization-IN-6 (化合物 5f) 是一种有效的微管蛋白聚合抑制剂,其IC50 为 1.09 μM。Tubulin polymerization-IN-6 抑制细胞迁移和管的形成,并有助于抗血管生成。Tubulin polymerization-IN-6 可显著抑制 HT29 移植 Balb/c 裸鼠肿瘤生长。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis | Protein Tyrosine Kinase/RTK
作用靶点:Microtubule/Tubulin | Apoptosis | ROS
In Vitro: Tubulin polymerization-IN-6 (compound 5f) (0-20 μM, 24 h) shows a broad spectrum of anti-proliferation activity against cancer cell lines.
Tubulin polymerization-IN-6 (0-100 nM, 24 h) inhibits tumor cells colony formation, up-regulates the expression of Ac-α-tubulin and DeY-α-tubulin .
Tubulin polymerization-IN-6 (0-5 μM, 1 h) competes with colchicine and directly binds to the colchicine binding site, thus inhibit tubulin polymerization.
Tubulin polymerization-IN-6 (0-250 nM, 24 h) possesses a favorable anti-migration activity against cancer cells.
Tubulin polymerization-IN-6 (0-50 nM, 24 h) has the ability to inhibit the angiogenesis of HUVEC cells.
Tubulin polymerization-IN-6 (0-100 nM, 24 h) induces cell cycle arrest by regulating associated proteins, induces apoptosis by regulating associated proteins and down-regulating mitochondrial membrane potential, and dose-dependently promotes the production of ROS in HT29 cells.
In Vivo: Tubulin polymerization-IN-6 (compound 5f) (HT29 xenograft Balb/c nude mice, 0-10 mg/kg, IP, once every two days, for three weeks) dose-dependently inhibits the tumor growth.
Tubulin polymerization-IN-6 (SD rats, 10 mg/kg, IV, once) shows the better pharmacokinetic properties.Pharmacokinetic Parameters of Tubulin polymerization-IN-6 in SD rats.
Parameters | 5f |
t1/2 (h) | 1.73 |
AUC (μg/Lh) | 5.67 |
MRT (h) | 1.92 |
CL (L/h/kg) | 1.76 |
Tmax (h) | 0.14 |
Cmax (ng/mL) | 6.88 |
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