Tubulin inhibitor 1
Based on 1 Customer Validation
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
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- Pureté : 99.81%
- CAS No.: 2237054-53-2
- Formule: C21H24N2O4
- Masse moléculaire:368.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
Tubulin[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
67 nM
Compound: 7a3
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Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
| CT26 | IC50 |
58 nM
Compound: 7a3
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Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK8 assay
Antiproliferative activity against mouse CT26 cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
| HeLa | IC50 |
32.8 nM
Compound: 7a3
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Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay
Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
| MCF7 | IC50 |
35.4 nM
Compound: 7a3
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Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
| MDA-MB-231 | IC50 |
0.031 μM
Compound: 7a3
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
| SK-OV-3 | IC50 |
0.017 μM
Compound: 7a3
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Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 assay
Antiproliferative activity against human SKOV3 cells after 72 hrs by CCK8 assay
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[PMID: 30006162] |
In Vitro
Tubulin inhibitor 1 (Compound 7a3) is a tubulin inhibitor, inhibits tubulin polymerization[1].
Tubulin inhibitor 1 has potent anti-proliferative activity against SK-OV-3, MDA-MB-231, HeLa, A549, CT26 and MCF-7 cells, with IC50s of 16.7 ± 3.0, 31.4 ± 0.7, 32.8 ± 2.9, 67.0 ± 0.8, 58.0 ± 2.4 and 35.4 ± 5.6 nM, respectively[1].
Tubulin inhibitor 1 (40, 80, and 160 nM, 48 hours) markedly causes cellular mitotic arrest in the G2/M phase, induces apoptosis in SK-OV-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:SK-OV-3 cells
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Concentration:40, 80, and 160 nM
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Incubation Time:48 h
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Result:Induced apoptosis in SK-OV-3 cells after treatment for 48 h.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old Balb/c nude mice (18-20 g) beraring SK-OV-3 cells[1]
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Dosage:50 mg/kg
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Administration:I.P., every two days three times for 20-25 days
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Result:Significantly reduced tumour growth in Balb/c nude mice bearing SK-OV-3 cells, without obvious body weight loss.
Chemical Information
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CAS No. 2237054-53-2
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Appearance Solid
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Masse moléculaire 368.43
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Formule C21H24N2O4
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Color White to off-white
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SMILES
CCOC1=CC=C(C2=CN(C)N=C2C3=CC(OC)=C(OC)C(OC)=C3)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
In Vitro:
DMSO : ≥ 125 mg/mL (339.28 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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.
Protocole
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
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- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7142 mL | 13.5711 mL | 27.1422 mL | 67.8555 mL |
| 5 mM | 0.5428 mL | 2.7142 mL | 5.4284 mL | 13.5711 mL | |
| 10 mM | 0.2714 mL | 1.3571 mL | 2.7142 mL | 6.7855 mL | |
| 15 mM | 0.1809 mL | 0.9047 mL | 1.8095 mL | 4.5237 mL | |
| 20 mM | 0.1357 mL | 0.6786 mL | 1.3571 mL | 3.3928 mL | |
| 25 mM | 0.1086 mL | 0.5428 mL | 1.0857 mL | 2.7142 mL | |
| 30 mM | 0.0905 mL | 0.4524 mL | 0.9047 mL | 2.2618 mL | |
| 40 mM | 0.0679 mL | 0.3393 mL | 0.6786 mL | 1.6964 mL | |
| 50 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3571 mL | |
| 60 mM | 0.0452 mL | 0.2262 mL | 0.4524 mL | 1.1309 mL | |
| 80 mM | 0.0339 mL | 0.1696 mL | 0.3393 mL | 0.8482 mL | |
| 100 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6786 mL |
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