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Tubulin polymerization-IN-6

CAS No. :

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.

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