Tubulin polymerization-IN-59
Based on 1 Customer Validation
Tubulin polymerization-IN-59 is a tubulin polymerization inhibitor and colchicine binding site inhibitor (CBSI) (IC50 = 6.1 μM). Tubulin polymerization-IN-59 exerts potent antiproliferative activity against cancer cells, while showing lower cytotoxicity to normal cells. Tubulin polymerization-IN-59 arrests colorectal cancer HCT 116 cells in G2/M phase, induces cell apoptosis, and suppresses tumor cell colony formation and migration. Tubulin polymerization-IN-59 can be used for the study of colorectal cancer (CRC).
For research use only. We do not sell to patients.
- Purity: 99.85%
- Formula: C20H21FO5
- Molecular Weight:360.38
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Apoptosis Compound Library
HY-L003
-
Cell Cycle/DNA Damage Compound Library
HY-L004
-
Anti-Cancer Compound Library
HY-L025
-
Anti-Aging Compound Library
HY-L034
-
Cytoskeleton Compound Library
HY-L060
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Protein-protein Interaction Inhibitor Library
HY-L109
-
Cell Death Library
HY-L162
-
MCE Bioactive Compound Library
HY-L001V
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
High-Efficiency Gene Editing Compound Library
HY-L244
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.59 μM
Compound: (R)-9k
|
Growth inhibition of human A2780 cells incubated for 1.5 hrs by MTT assay
Growth inhibition of human A2780 cells incubated for 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| CT26 | IC50 |
4.11 μM
Compound: (R)-9k
|
Growth inhibition of CT26 cells incubated for 1.5 hrs by MTT assay
Growth inhibition of CT26 cells incubated for 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| HCT-116 | IC50 |
0.26 μM
Compound: (R)-9k
|
Growth inhibition of human HCT-116 cells incubated for 1.5 hrs by MTT assay
Growth inhibition of human HCT-116 cells incubated for 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| HEK293 | IC50 |
7.45 μM
Compound: (R)-9k
|
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated 1.5 hrs by MTT assay
Cytotoxicity against HEK293 cells assessed as inhibition of cell growth incubated 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| HeLa | IC50 |
0.38 μM
Compound: (R)-9k
|
Growth inhibition of human HeLa cells incubated for 1.5 hrs by MTT assay
Growth inhibition of human HeLa cells incubated for 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| HUVEC | IC50 |
15.01 μM
Compound: (R)-9k
|
Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth incubated 1.5 hrs by MTT assay
Cytotoxicity against human HUVEC cells assessed as inhibition of cell growth incubated 1.5 hrs by MTT assay
|
[PMID: 38107178] |
| SW480 | IC50 |
1.31 μM
Compound: (R)-9k
|
Growth inhibition of human SW480 cells incubated for 1.5 hrs by MTT assay
Growth inhibition of human SW480 cells incubated for 1.5 hrs by MTT assay
|
[PMID: 38107178] |
Tubulin polymerization-IN-59 ((R)-9k) (48-72 h) exerts potent antiproliferative activity against HeLa, A2780, HCT 116, SW480, and CT-26 cells, with IC50 values of 0.38 μM, 0.59 μM, 0.26 μM, 1.31 μM, and 4.11 μM, respectively[1].
Tubulin polymerization-IN-59 (3-12 μM) inhibits tubulin polymerization in a dose-dependent manner, with an IC50 value of 6.1 μM[1].
Tubulin polymerization-IN-59 (1-25 μM, 3.5 h) reduces the formation of EBI-β-tubulin adduct in HCT 116 cells by competing for the colchicine binding site on tubulin[1].
Tubulin polymerization-IN-59 (1.5-6.0 μM, 24 h) arrests HCT 116 cells in the G2/M phase in a dose-dependent manner and induces apoptosis of HCT 116 cells[1].
Tubulin polymerization-IN-59 (0.1-2 μM, 2 weeks) inhibits colony formation of HCT 116 cells[1].
Tubulin polymerization-IN-59 (0.5-5.0 μM, 24 h) inhibits migration of HCT 116 cells in a dose-dependent manner
Tubulin polymerization-IN-59 (0.16-40 μM) weakly inhibits the hERG potassium channel in CHO cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:HCT 116 cells
-
Concentration:1.5, 3, 6.0 μM
-
Incubation Time:24 h
-
Result:Arrested HCT 116 cells in the G2/M phase in a dose-dependent manner.
-
Cell Line:HCT 116 cells
-
Concentration:1.5, 3, 6.0 μM
-
Incubation Time:24 h
-
Result:Induced apoptosis of HCT 116 cells.
Chemical Information
-
Appearance Solid
-
Molecular Weight 360.38
-
Formula C20H21FO5
-
Color White to off-white
-
SMILES
CCOC1=CC=C(C=C1F)[C@H]2CC(C3=CC(OC)=C(C(OC)=C32)OC)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (277.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
-
Data Sheet (280 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7748 mL | 13.8742 mL | 27.7485 mL | 69.3712 mL |
| 5 mM | 0.5550 mL | 2.7748 mL | 5.5497 mL | 13.8742 mL | |
| 10 mM | 0.2775 mL | 1.3874 mL | 2.7748 mL | 6.9371 mL | |
| 15 mM | 0.1850 mL | 0.9249 mL | 1.8499 mL | 4.6247 mL | |
| 20 mM | 0.1387 mL | 0.6937 mL | 1.3874 mL | 3.4686 mL | |
| 25 mM | 0.1110 mL | 0.5550 mL | 1.1099 mL | 2.7748 mL | |
| 30 mM | 0.0925 mL | 0.4625 mL | 0.9249 mL | 2.3124 mL | |
| 40 mM | 0.0694 mL | 0.3469 mL | 0.6937 mL | 1.7343 mL | |
| 50 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3874 mL | |
| 60 mM | 0.0462 mL | 0.2312 mL | 0.4625 mL | 1.1562 mL | |
| 80 mM | 0.0347 mL | 0.1734 mL | 0.3469 mL | 0.8671 mL | |
| 100 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6937 mL |
Tubulin polymerization-IN-59 Related Classifications
HY-157543 Related Classifications
Powered by Bioz