Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor (IC 50 = 3.15 μM) that exhibits potent anti-vascular and anticancer activities including cancer cell apoptosis [1].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 1,520.00 | |
50 mg | 6-8 weeks | $ 1,980.00 | |
100 mg | 6-8 weeks | $ 2,500.00 |
Description | Tubulin polymerization-IN-14 (Compound 20a) is a tubulin polymerization inhibitor (IC 50 = 3.15 μM) that exhibits potent anti-vascular and anticancer activities including cancer cell apoptosis [1]. |
In vitro | Tubulin polymerization-IN-14 (Compound 20a) targets the colchicine binding site on tubulin to inhibit cancer cell growth at concentrations of 0-1 μM over 72 hours, as per studies. At lower concentrations (5-20 nM) over 48 hours, this compound halts the cell cycle in the G2/M phase and significantly triggers apoptosis in K562 cells in a dose-dependent manner. It also leads to mitochondrial membrane potential collapse and mitochondrial dysfunction. Furthermore, at similar concentrations (5-20 nM) but over a shorter period (24 hours), Tubulin polymerization-IN-14 notably reduces wound closure and the formation of capillary-like structures in HUVECs, evidencing its potential to inhibit angiogenesis, again in a concentration-dependent fashion. Additional assays underscore its potency: an anti-proliferative effect with an IC 50 of 0.01 ± 0.001 μM against K562 cells, cytotoxic activities against a panel of cell lines including HepG2, HCT-8, MDA-MB-231, and HFL-1 with IC 50 values ranging from 0.019 to 0.118 μM. Cell cycle analysis revealed a concentration-dependent increase in G2/M phase arrest, and apoptosis analysis showed a significant increase in apoptotic cells after treatment, indicating its effectiveness in inducing programmed cell death. Lastly, cell migration assays in HUVECs demonstrated a significant dose-dependent decrease in cell migration, highlighting its role in inhibiting cellular movements associated with metastasis. |
In vivo | Tubulin polymerization-IN-14 (Compound 20a), administered intravenously at dosages of 15 and 30 mg/kg daily for 21 days, exhibited a marked and dose-dependent anti-tumor effect in a liver tumor allograft mouse model (Five-week-old male ICR mice), demonstrating significant tumor weight reduction by 68.7% at the 30 mg/kg dosage without evident toxicity or significant body weight loss [1]. |
Molecular Weight | 290.74 |
Formula | C15H15ClN2O2 |
CAS No. | 2417134-05-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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Tubulin polymerization-IN-14 2417134-05-3 inhibitor inhibit