Colchicine is a natural product extracted from Colchicum spp. It is also a tubulin inhibitor and microtubule disruptor with an IC50 of 3 nM for inhibition of microtubule polymerization, and a competitive antagonist of α3 glycine receptors (GlyRs). Colchicine is also a competitive antagonist of α3 Glycine receptors (GlyRs) and has been used in gout research.
 |
Source | Cancer Res (2017). Figure 2. Colchicine |
| Method | Scratch migration assay | |
| Cell Lines | A375 and RPMI7951 cells | |
| Concentrations | 25 nM | |
| Incubation Time | 12 and 24 h | |
| Results | The effect of DJ101 on A375 cell colony formation was similar to colchicine at the same concentration, which had colonies covering a total area of 34.7% ± 1.5% |
| Cell Experiment | |
|---|---|
| Cell lines | COS-7 cells |
| Preparation method | After 20 min, the samples were mixed with 5 nM CT20126, colchicine or Taxol and incubated at 37 °C for 5 min. The samples were cooled in an ice bath for depolymerization (still within the light path cell). Successive reactions were performed for another 25 min at 37 °C. |
| Concentrations | 5 nM |
| Incubation time | 5 min |
| Animal Experiment | |
|---|---|
| Animal models | Male Sprague–Dawley rats |
| Formulation | water |
| Dosages | 5 mg/kg |
| Administration | gavage |
| Molecular Weight | 399.44 |
| Formula | C22H25NO6 |
| CAS Number | 64-86-8 |
| Solubility (25°C) | DMSO 45 mg/mL Water 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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