Colchicine

Biological Activity

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.

Customer Product Validations & Biological Datas

	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%

Protocol (for reference only)

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

Chemical Information

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

Conversion of different model animals based on BSA (PMID: 27057123)

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 K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Peake PW, et al. Clin Toxicol (Phila). Fab fragments of ovine antibody to colchicine enhance its clearance in the rat.

[2] Kim SK, et al. Exp Mol Med. The colchicine derivative CT20126 shows a novel microtubule-modulating activity with apoptosis.