Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tubulin polymerization-IN-4 is an effective inhibitor of tubulin polymerization (IC50=4.6 μM)。 Tubulin polymerization-IN-4 can destroy tubulin polymerization, block cell cycle at G2/M phase, induce apoptosis, and inhibit cell cloning and migration. Tubulin polymerization-IN-4 can also damage the vascular system.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 10-14 weeks | $ 1,520.00 | |
50 mg | 10-14 weeks | $ 1,980.00 | |
100 mg | 10-14 weeks | $ 2,500.00 |
Description | Tubulin polymerization-IN-4 is an effective inhibitor of tubulin polymerization (IC50=4.6 μM)。 Tubulin polymerization-IN-4 can destroy tubulin polymerization, block cell cycle at G2/M phase, induce apoptosis, and inhibit cell cloning and migration. Tubulin polymerization-IN-4 can also damage the vascular system. |
In vitro | Tubulin polymerization-IN-4 (compound 9j) demonstrates a range of inhibitory effects on cancer cell activity and tubulin polymerization, showcasing its therapeutic potential. At concentrations between 0-1 μM over 48 hours, it exerts sub-micromolar inhibitory activities against HeLa, SiHa, and MS751 cell lines, with specific IC50 values indicating its efficacy. Moreover, within a short span of 0-20 minutes at increased concentrations (3, 6, and 12.5 μM), the compound inhibits tubulin polymerization in a dose-dependent manner, marked by 39%, 54%, and 77% inhibition at respective concentrations. Additionally, it hinders the formation of EBI-β-tubulin adduct and disrupts the vascular tube formation by HUVEC cells, indicating its potential effects on tumor angiogenesis and cellular structuring. Notably, at low micromolar ranges (0.1-0.4 μM over 24 hours), Tubulin polymerization-IN-4 alters cell cycle distribution towards the G2/M phase, triggers apoptosis in HeLa cells, and effectively inhibits HeLa cell migration and colony formation, illustrating its multifaceted antitumor activities. Furthermore, its cytotoxicity assay in HK-2 cells confirms a favorable renal safety profile, with an IC50 of 188 ± 16 μM, showcasing its therapeutic safety margin. These findings collectively underscore the compound's potential as a cancer therapeutic agent with a well-defined mechanism of action and acceptable safety profile. |
In vivo | Tubulin polymerization-IN-4, administered intraperitoneally (IP) at doses ranging from 100 to 1000 mg/kg, exhibits very low toxicity, with its lethal dose 50 (LD50) exceeding 1000 mg/kg [1]. When given daily for 21 days at doses of 30 and 60 mg/kg, it effectively inhibits tumor growth, achieving tumor growth inhibition (TGI) rates of 35% and 58%, respectively, at these doses [1]. Furthermore, a single IP administration of Tubulin polymerization-IN-4 at 30 mg/kg demonstrates moderate pharmacokinetic properties, with detailed parameters in ICR mice including a half-life (T 1/2) of 1.56 ± 0.28 hours, a time to reach maximum concentration (T max) of 0.25 hours, a maximum concentration (C max) of 6215 ± 308 μg/L, an area under the curve from 0 to last measurable concentration (AUC 0-t) of 5609 ± 347 μg/L·h, an area under the curve from 0 to infinity (AUC 0-∞) of 5940 ± 347 μg/L·h, a volume of distribution (V Z /F) of 11.35 ± 1.29 L/kg, a clearance rate (CL Z /F) of 5.05 ± 0.91 L/h/kg, and a mean residence time (MRT) of 1.77 ± 0.43 hours [1]. |
Molecular Weight | 400.86 |
Formula | C21H21ClN2O4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Tubulin polymerization-IN-4 inhibitor inhibit