Tubulin inhibitor 11
Based on 1 Customer Validation
Tubulin inhibitor 11 is a potent and orally active tubulin inhibitor. Tubulin inhibitor 11 targets the Colchicine binding site on tubulin, inhibits tubulin polymerization, promotes mitotic blockade and apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.76%
- CAS No.: 2366260-33-3
- Formula: C22H23N3O3S
- Molecular Weight:409.50
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.025 μM
Compound: 48
|
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| A549 | IC50 |
0.03 μM
Compound: 48
|
Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against paclitaxel-resistant human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| B16-F10 | IC50 |
0.002 μM
Compound: 48
|
Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| BGC-823 | IC50 |
0.021 μM
Compound: 48
|
Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| DU-145 | IC50 |
0.004 μM
Compound: 48
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 96 hrs by real-time cell analysis
|
[PMID: 36511661] |
| DU-145 | IC50 |
0.008 μM
Compound: 48
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| DU-145 | IC50 |
0.009 μM
Compound: 48
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by real-time cell analysis
|
[PMID: 36511661] |
| DU-145 | IC50 |
0.01 μM
Compound: 48
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 24 hrs by real-time cell analysis
|
[PMID: 36511661] |
| DU-145 | IC50 |
0.01 μM
Compound: 48
|
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis
Antiproliferative activity against human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by real-time cell analysis
|
[PMID: 36511661] |
| HCT-116 | IC50 |
0.004 μM
Compound: 48
|
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| HCT-8 | IC50 |
0.022 μM
Compound: 48
|
Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HCT-8 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| HepG2 | IC50 |
0.003 μM
Compound: 48
|
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HepG2 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| HGC-27 | IC50 |
0.006 μM
Compound: 48
|
Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human HGC-27 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| HUVEC | IC50 |
0.032 μM
Compound: 48
|
Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Anti-angiogenesis activity against HUVEC cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| MCF7 | IC50 |
0.006 μM
Compound: 48
|
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| MCF7R | IC50 |
0.014 μM
Compound: 48
|
Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against paclitaxel-resistant human MCF7R cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| MDA-MB-231 | IC50 |
0.009 μM
Compound: 48
|
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| NCI-H1299 | IC50 |
0.004 μM
Compound: 48
|
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| NCI-H1437 | IC50 |
0.002 μM
Compound: 48
|
Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1437 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| NCI-H460 | IC50 |
0.077 μM
Compound: 48
|
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| SW1990 | IC50 |
0.015 μM
Compound: 48
|
Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SW1990 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
|
[PMID: 36511661] |
| Vero | IC50 |
0.04 μM
Compound: 48
|
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs
Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 48 hrs
|
[PMID: 36511661] |
Tubulin inhibitor 11 (Compound 48; 0.03-0.1 μM; 12 hours) causes cell cycle arrest at G2/M phase. Tubulin inhibitor 11 reduces cdc2 phosphorylation and increases cyclin B1 and phosphorylation of histone H3 at Ser10 in cells[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM; 48 hours) causes cancer cell apoptosis[1].
Tubulin inhibitor 11 (Compound 48) demonstrates favorable antiproliferative activities in DU145 cells with an IC50 of 8 nM[1].
Tubulin inhibitor 11 (Compound 48; 0.03-0.3 μM) significantly reduces the expression levels of acetyl-α-tubulin and α-tubulin in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:DU145 cells
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Concentration:0.01 μM, 0.03 μM, and 0.1 μM
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Incubation Time:12 hours
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Result:Caused cell cycle arrest at G2/M phase.
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Cell Line:DU145 cells
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Concentration:0.03 μM, 0.1 μM, and 0.3 μM
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Incubation Time:48 hours
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Result:Induced cancer cell apoptosis.
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Cell Line:DU145 cells
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Concentration:0.01 μM, 0.03 μM, and 0.1 μM
-
Incubation Time:12 hours
-
Result:Reduced cdc2 phosphorylation and increased cyclin B1 and phosphorylation of histone H3 at Ser10 in cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male athymic BALB/c nude mice (18-20 g) injected with DU145, NCI-H1299 or A549R cells[1]
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Dosage:5 mg/kg, 10 mg/kg
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Administration:p.o; once daily
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Result:Effectively suppressed tumor growth.
Chemical Information
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CAS No. 2366260-33-3
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Appearance Solid
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Molecular Weight 409.50
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Formula C22H23N3O3S
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Color Off-white to pink
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SMILES
O=C(C1=CC=C(C(NS(C2=CC=C(C=C2)C)(=O)=O)=C1)C)NCC3=CN=C(C=C3)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 (244.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (6.11 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.11 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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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 | 2.4420 mL | 12.2100 mL | 24.4200 mL | 61.0501 mL |
| 5 mM | 0.4884 mL | 2.4420 mL | 4.8840 mL | 12.2100 mL | |
| 10 mM | 0.2442 mL | 1.2210 mL | 2.4420 mL | 6.1050 mL | |
| 15 mM | 0.1628 mL | 0.8140 mL | 1.6280 mL | 4.0700 mL | |
| 20 mM | 0.1221 mL | 0.6105 mL | 1.2210 mL | 3.0525 mL | |
| 25 mM | 0.0977 mL | 0.4884 mL | 0.9768 mL | 2.4420 mL | |
| 30 mM | 0.0814 mL | 0.4070 mL | 0.8140 mL | 2.0350 mL | |
| 40 mM | 0.0611 mL | 0.3053 mL | 0.6105 mL | 1.5263 mL | |
| 50 mM | 0.0488 mL | 0.2442 mL | 0.4884 mL | 1.2210 mL | |
| 60 mM | 0.0407 mL | 0.2035 mL | 0.4070 mL | 1.0175 mL | |
| 80 mM | 0.0305 mL | 0.1526 mL | 0.3053 mL | 0.7631 mL | |
| 100 mM | 0.0244 mL | 0.1221 mL | 0.2442 mL | 0.6105 mL |