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Tubulin polymerization-IN-4

CAS No. :

MCE 站：Tubulin polymerization-IN-4

产品活性：Tubulin polymerization-IN-4 是一种有效的微管蛋白聚合体 (tubulin polymerization) 抑制剂，IC₅₀ 为 4.6 μM。Tubulin polymerization-IN-4 对HeLa细胞可破坏微管蛋白聚合和血管系统，将细胞周期阻滞在G2/M期，诱导细胞凋亡 (apoptosis)，抑制细胞的克隆发生和迁移。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Apoptosis

In Vitro: Tubulin polymerization-IN-4 (compound 9j) (0-1 μM; 48 hours) exhibits sub-micromolar inhibitory activities against HeLa, SiHa ａnd MS751.
Tubulin polymerization-IN-4 (3, 6 ａnd 12.5 μM; 0-20 min) inhibits tubulin polymerization in a concentration-dependent manner with the inhibition percentages of 39%, 54%, ａnd 77% at 3, 6 ａnd 12.5 μM.
Tubulin polymerization-IN-4 (1-100 μM; 2 hours) inhibits the formation of EBI-β-tubulin adduct in a concentration-dependent manner.
Tubulin polymerization-IN-4 (0.2 μM; 1 ａnd 2 hours) disrupts the HUVEC-formed vascular tube.
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) increases cell distribution to the G2/M phase in a concentration-dependent manner.
Tubulin polymerization-IN-4 (0.1-0.4 μM; 24 hours) induces apoptosis of HeLa cells.
Tubulin polymerization-IN-4 (20, 50, 100 nM; 14 days) reduces new colony formation ａnd suppresses HeLa cell growth for 14 days in a dose-dependent manner.
Tubulin polymerization-IN-4 (0.1, 0.2 ａnd 0.4 μM; 24 hours) effectively inhibits the migration of HeLa cells in a concentration-dependent manner.
Tubulin polymerization-IN-4 (0-200 μM; 24 hours) exhibits good renal safety profile, with IC₅₀ of 188 ± 16 μM in HK-2 cells.

In Vivo: Tubulin polymerization-IN-4 (100-1000 mg/kg; IP, single) exhibits extremely low toxicity with LD₅₀ over 1000 mg/kg.
Tubulin polymerization-IN-4 (30 ａnd 60 mg/kg; IP; daily for 21 days) inhibits the tumor growth, with TGI of 35% ａnd 58% at dosing 30 ａnd 60 mg/kg.
Tubulin polymerization-IN-4 (30 mg/kg; IP; single) presents the modest pharmacokinetic properties.
Pharmacokinetic Parameters of Tubulin polymerization-IN-4 in ICR mice.

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