Combretastatin A4 inhibits tubulin polymerization at the colchicine-binding site of beta-tubulin. Combretastatin A4 has antitumor activity by inhibiting AKT function in human gastric cells. The inhibited AKT activation causes decreased cell proliferation, cell cycle arrest, and reduced in vitro migration/invasiveness and in vivo metastatic ability.
| Cell Experiment | |
|---|---|
| Cell lines | MDA-MB-231, A549, and Hela cells |
| Preparation method | Growing MDA-MB-231, A549, and HeLa cells in DMEM medium (115 units/mL of penicillin G, 115 μg/mL of streptomycin, and 10% fetal bovine serum). Seeding cells in 96-well plates (5000 cells/well) containing 50 μL of growth medium for 24 h. After medium removal, adding 100 μL of fresh medium containing individual analogue compounds at different concentrations to each well and incubating at 37 ℃ for 72 h. After 24 h of culture, supplementing the cells with 50 μL of analogue compounds dissolved in DMSO (less than 0.25% in each preparation). After 72 h of incubation, adding 20 μL of resazurin for 2 h before recording fluorescence at 560 nm (excitation) and 590 nm (emission) using a Victor microtiter plate fluorimeter. Defining the IC50 as the compound concentration required to inhibit cell proliferation by 50% in comparison with cells treated with the maximum amount of DMSO (0.25%) and considered as 100% viability. |
| Concentrations | ~3.8 nM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | FVB/N or nude NMRI female mice bearing NT2 and MDA-MB-231 tumors |
| Formulation | DMSO |
| Dosages | 100 mg/kg |
| Administration | i.p. |
| Molecular Weight | 316.35 |
| Formula | C18H20O5 |
| CAS Number | 117048-59-6 |
| Solubility (25°C) | 100 mM in ethanol 100 mM in DMSO |
| 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.
| Related Microtubule Products |
|---|
| P34cdc2 Kinase Fragment
P34cdc2 Kinase Fragment is associated with the completion of DNA replication in yeast mitosis. |
| Cemadotin
Cemadotin (LU103793) is an analogue of Dolastatin 15 which is naturally occurring cytotoxic peptides. |
| VLS-1488
VLS-1488 is an orally active KIF18A inhibitor that inhibits KIF18A microtubule-dependent ATPase activity with an IC50 value of 0.016 μM. |
| ENMD-1198
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. |
| Tubulin/JAK2-IN-1
Tubulin/JAK2-IN-1 is a dual inhibitor of Janus kinase 2 (JAK2) and microtubule. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
