| Size | Price | |
|---|---|---|
| 10mg | ||
| 50mg | ||
| 100mg | ||
| Other Sizes |
| Targets |
Microtubule/Tubulin
|
|---|---|
| ln Vitro |
4-Formylcolchicine (compound 7) exhibits antiproliferative action against A549, HT-29, and HCT116 cells, with IC50s of 1.007, 0.128, and 0.054 µM, respectively[1].
|
| ln Vivo |
Liver fibrosis was induced by chronically (7 weeks) administering CCl4, to rats. Animals were divided into four groups: (a) controls, (b) treated with CCI, alone, (c) treated with CCl4 and colchicine and (d) treated with CCl4 and 4-Formylcolchicine bound to lactosaminated serum albumin (FC-LASA). Liver dysfunction was monitored by biochemical tests (alkaline phosphatase [ALP], γ-glutamyltransferase [γGT], aspartate and alanine transaminases [AST and ALT], albumin and total bilirubin). Fibrosis was evaluated by determining hydroxyproline and by microscopic examination. The exposure to CCl4 produced major alterations of liver structure and collagen deposition. These effects were partially counteracted by colchicine and to a greater extent by FC-LASA. Morphological findings paralleled biochemical data. The information reported here indicates that colchicine has an antifibrotic activity on the liver of intoxicated rats and that FC-LASA is more active than colchicine itself as an antifibrotic agent [1].
|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: A549, HT-29, HCT116 cells Tested Concentrations: 0-5 µM Incubation Duration: 24 h Experimental Results: Inhibited cell growth with IC50s of 1.007, 0.128, 0.054 µM for A549, HT-29, HCT116 cells, respectively. |
| Animal Protocol |
Effect of colchicine and its derivatives on liver fibrosis [1]
To study the effects of colchicine derivatives on liver fibrosis in vivo, we used adult Sprague-Dawley male rats (about 250 g body wt.). The animals were divided into four groups. (A) Controls received 2 ml.kg-1 body wt. mineral oil by intraperitoneal route and 250 ~tl of saline by injection into the tail vein three times a week for 7 weeks; (B) Animals were intoxicated with carbon tetrachloride. They were treated as those of groups A, except that they received a mixture of mineral oil and carbon tetrachloride (65:35 v/v, 2 ml'kg-1 body wt.); (C) The animals belonging to this group were treated as those of group B but they received colchicine (120 ~tg-kg-1 body wt., dissolved in saline) instead of saline; and (D) animals were treated as in (C), but colchicine was replaced by FC-LASA (120 ~tg.kg-~ body wt., as free colchicine). Doses were adjusted to body wt. and expressed as free colchicine. Owing to the high toxicity of CC14 (only about 40-50% of the animals survived 7 weeks' treatment), we began the experiment with 50 animals (various treatments) and 15 animals (controls), to have the final number of animals reported in Table 1. At the end of the experiment, animals were anaesthetised with diethyl ether and their blood was drained by heart puncture and collected in pre-heparinated vessels. Plasma was prepared by centrifugation at 1000 x g for 10 min and some biochemical parameters (alkaline phosphatase (ALP), aspartate and alanine transaminases (AST and ALT) y-glutamyl transferase (yGT), albumin and total bilirubin) were determined by commercial kits. Livers were used to verify collagen content (as hydroxyproline) and for histological examination. |
| References |
|
| Additional Infomation |
Histological results were consistent with biochemical results, especially with the determination of hepatic hydroxyproline, which was more accurate than microscopic assessment in reflecting the degree of liver fibrosis. All tests showed that FC-LASA was more effective than colchicine in reducing liver fibrosis in rats after CC14 administration. [1] We prepared novel colchicine derivatives with different substituents at the C4 position. Among them, the 4-halogenated derivatives 3-6 showed higher activity than colchicine in cancer cell lines (A549, HT29, HCT116) and in mice transplanted with the HCT116 human colorectal cancer cell line (1). In addition, we prepared prodrugs with dipeptide side chains using 4-substituted colchicine and confirmed that these prodrugs could be activated by the overexpressed enzyme cathepsin B in tumor cells and had selective toxicity to tumor cells. [2]
|
| Molecular Formula |
C23H25NO7
|
|---|---|
| Molecular Weight |
427.45
|
| Exact Mass |
427.163
|
| CAS # |
2730-82-7
|
| PubChem CID |
332237
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.29g/cm3
|
| Boiling Point |
786.9ºC at 760mmHg
|
| Flash Point |
429.7ºC
|
| Vapour Pressure |
9.93E-25mmHg at 25°C
|
| Index of Refraction |
1.589
|
| LogP |
3.075
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
31
|
| Complexity |
815
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(=O)N[C@H]1CCC2=C(C(=C(C(=C2C3=CC=C(C(=O)C=C13)OC)OC)OC)OC)C=O
|
| InChi Key |
JUWAUXATKRGHCK-KRWDZBQOSA-N
|
| InChi Code |
InChI=1S/C23H25NO7/c1-12(26)24-17-8-6-14-16(11-25)21(29-3)23(31-5)22(30-4)20(14)13-7-9-19(28-2)18(27)10-15(13)17/h7,9-11,17H,6,8H2,1-5H3,(H,24,26)/t17-/m0/s1
|
| Chemical Name |
N-[(7S)-4-formyl-1,2,3,10-tetramethoxy-9-oxo-6,7-dihydro-5H-benzo[a]heptalen-7-yl]acetamide
|
| Synonyms |
4-Formylcolchicine; 2730-82-7; NSC328403; NSC-328403; CHEMBL155693; DTXSID30950024;
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 160 mg/mL (374.31 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (5.85 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3395 mL | 11.6973 mL | 23.3945 mL | |
| 5 mM | 0.4679 mL | 2.3395 mL | 4.6789 mL | |
| 10 mM | 0.2339 mL | 1.1697 mL | 2.3395 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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