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2478584-74-4
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αβ-Tubulin-IN-1
CAS No. : 2478584-74-4
MCE 国际站：αβ-Tubulin-IN-1
产品活性：αβ-Tubulin-IN-1 是一种有效且具有口服活性的 αβ-Tubulin 抑制剂。αβ-Tubulin-IN-1 诱导细胞周期停滞在 G2/M 期和诱导细胞凋亡 (apoptosis)。αβ-Tubulin-IN-1 抑制肿瘤细胞迁移和转移。αβ-Tubulin-IN-1 以剂量依赖性方式显示出显着的抗肿瘤功效。
研究领域：Apoptosis | Cytoskeleton | Cell Cycle/DNA Damage
作用靶点：Apoptosis | Microtubule/Tubulin
In Vitro: αβ-Tubulin-IN-1 (compound 12 b) (0, 0.5, 1, 5, 10, 50 µM; 16 h) promotes αβ-tubulin degradation in a concentration-dependent manner in Hela and K562 (0-10 µM) cells.
αβ-Tubulin-IN-1 exhibits potent cytotoxic activity toward sensitive cells and resistant cells.
αβ-Tubulin-IN-1 (0-300 nM; 48 h) induces cell cycle arrest at G2/M and efficient apoptosis in A2780S and A2780T cells.
αβ-Tubulin-IN-1 (0, 1.25, 2.5, 5, 10 nM; 24, 48 h) inhibits tumor cell migration and Metastasis with the inhibition rate of 76.21% and 85.07% for 24 , 48 h in human umbilical vein endothelial cells (HUVEC).
In Vivo: αβ-Tubulin-IN-1 (5 mg/kg; i.v., p.o.) shows intravenous and oral administration approaches are available in vivo.
αβ-Tubulin-IN-1 (10, 20, 40 mg/kg; i.v.; 3 times a week for 2-4 weeks) shows significant antitumor efficacy in a dose dependent manner.
Pharmacokinetic Parameters of αβ-Tubulin-IN-1 in rats.
| route | i.v. | p.o. |
| dose (mg/kg) | 5 | 5 |
| T1/2 (h) | 3.57±1.10 | 4.42±1.90 |
| CL (L/h/kg) | 1.52±0.39 | 5.06±1.70 |
| Vss (L/kg) | 8.08±4.19 | 35.26±25.76 |
| AUC0-∞ (µg/mL·h) | 3448.81±782.66 | 1058.74±285.62 |
| Cmax (µg/L) | 2601.47±444.20 | 189.29±119.02 |
| F (%) | 30.70 |
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