Batabulin
Based on 1 Customer Validation
Batabulin (T138067) is an antitumor agent, which binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Batabulin affects cell morphology and leads to cell-cycle arrest ultimately induces apoptotic cell death.
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- Purity: 99.89%
- CAS No.: 195533-53-0
- 화학식: C13H7F6NO3S
- 분자량:371.26
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
β-tubulin[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | IC50 |
>40 μM
Compound: T138067
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Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
Cytotoxicity against human BEAS2B cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
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[PMID: 29471119] |
| BEAS-2B | IC50 |
12.2 μM
Compound: T138067
|
Antiproliferative activity against human BEAS2B cells after 70 hrs by alamar blue assay
Antiproliferative activity against human BEAS2B cells after 70 hrs by alamar blue assay
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[PMID: 29471119] |
| DLD-1 | EC50 |
0.15 μM
Compound: 11
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Tested for caspase activation activity in colorectal DLD-1 cell line
Tested for caspase activation activity in colorectal DLD-1 cell line
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[PMID: 12773051] |
| HBL-100 | IC50 |
>40 μM
Compound: T138067
|
Cytotoxicity against human HBL100 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
Cytotoxicity against human HBL100 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
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[PMID: 29471119] |
| HBL-100 | IC50 |
0.2 μM
Compound: T138067
|
Antiproliferative activity against human HBL100 cells after 70 hrs by alamar blue assay
Antiproliferative activity against human HBL100 cells after 70 hrs by alamar blue assay
|
[PMID: 29471119] |
| HeLa | IC50 |
101 nM
Compound: T-138067
|
Inhibition of growth of human cervical carcinoma (HeLa) cell line.
Inhibition of growth of human cervical carcinoma (HeLa) cell line.
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[PMID: 11606124] |
| HUVEC | IC50 |
16.4 μM
Compound: T138067
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Cytotoxicity against HUVEC assessed as reduction in cell viability after 70 hrs by alamar blue assay
Cytotoxicity against HUVEC assessed as reduction in cell viability after 70 hrs by alamar blue assay
|
[PMID: 29471119] |
| HUVEC | IC50 |
6.3 μM
Compound: T138067
|
Antiproliferative activity against HUVEC after 70 hrs by alamar blue assay
Antiproliferative activity against HUVEC after 70 hrs by alamar blue assay
|
[PMID: 29471119] |
| MDR | IC50 |
87 nM
Compound: T-138067
|
Inhibition of growth of human mammary carcinoma (MCF-7) cell line that exhibits the MDR phenotype.
Inhibition of growth of human mammary carcinoma (MCF-7) cell line that exhibits the MDR phenotype.
|
[PMID: 11606124] |
| MIA PaCa-2 | IC50 |
47.3 μM
Compound: T138067
|
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
Cytotoxicity against human MIAPaCa2 cells assessed as reduction in cell viability after 70 hrs by alamar blue assay
|
[PMID: 29471119] |
| T47D | EC50 |
0.17 μM
Compound: 11
|
Tested for caspase activation activity in human breast cancer T47D cells
Tested for caspase activation activity in human breast cancer T47D cells
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[PMID: 12773051] |
| ZR-75-1 | EC50 |
0.13 μM
Compound: 11
|
Tested for caspase activation activity in human breast cancer ZR-75-1 cells
Tested for caspase activation activity in human breast cancer ZR-75-1 cells
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[PMID: 12773051] |
Batabulin (T138067; 30-300 nM; 24 hours; MCF7 cells) treatment shows approximately 25-30% tetraploid (4n) DNA content in cells, indicating an arrest at the G2/M cell-cycle boundary[1].
Batabulin (T138067; 30-300 nM; 24-48 hours; MCF7 cells) treatment shows 25-30% apoptosis. After a 48-hr exposure to 100 nM Batabulin, approximately 50-80% of the cell population is undergoing apoptosis[1].
Batabulin (T138067) binds covalently and selectively to a subset of the β-tubulin isotypes, thereby disrupting microtubule polymerization. Covalent modification occurs at a conserved Cys-239 shared by the β1, β2, and β4 tubulin isotypes. Cells exposed to Batabulin become altered in shape, indicating a collapse of the cytoskeleton, and show an increase in chromosomal ploidy[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 cells
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Concentration:30 nM, 100 nM and 300 nM
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Incubation Time:24 hours
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Result:Showed an arrest at the G2/M cell-cycle boundary.
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Cell Line:MCF7 cells
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Concentration:30 nM, 100 nM and 300 nM
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Incubation Time:24 hours or 48 hours
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Result:25-30% of cells showed the reduced DNA content characteristic of apoptotic 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 nude mice (nu/nu) (6-8 week-old, 20-25 g) injected with CCRF-CEM cells[1]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; once per week; on days 5, 12, and 19
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Result:Impaired the growth of the drug-sensitive CCRF-CEM tumors.
Chemical Information
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CAS No. 195533-53-0
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Appearance Solid
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분자량 371.26
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화학식 C13H7F6NO3S
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Color White to off-white
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SMILES
O=S(C1=C(F)C(F)=C(F)C(F)=C1F)(NC2=CC=C(OC)C(F)=C2)=O
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Synonyms
T138067
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
Ethanol : 100 mg/mL (269.35 mM; Need ultrasonic)
DMSO : 100 mg/mL (269.35 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 (6.73 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 (6.73 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.
순도&문서
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 |
|---|---|---|---|---|---|
| Ethanol / DMSO | 1 mM | 2.6935 mL | 13.4677 mL | 26.9353 mL | 67.3383 mL |
| 5 mM | 0.5387 mL | 2.6935 mL | 5.3871 mL | 13.4677 mL | |
| 10 mM | 0.2694 mL | 1.3468 mL | 2.6935 mL | 6.7338 mL | |
| 15 mM | 0.1796 mL | 0.8978 mL | 1.7957 mL | 4.4892 mL | |
| 20 mM | 0.1347 mL | 0.6734 mL | 1.3468 mL | 3.3669 mL | |
| 25 mM | 0.1077 mL | 0.5387 mL | 1.0774 mL | 2.6935 mL | |
| 30 mM | 0.0898 mL | 0.4489 mL | 0.8978 mL | 2.2446 mL | |
| 40 mM | 0.0673 mL | 0.3367 mL | 0.6734 mL | 1.6835 mL | |
| 50 mM | 0.0539 mL | 0.2694 mL | 0.5387 mL | 1.3468 mL | |
| 60 mM | 0.0449 mL | 0.2245 mL | 0.4489 mL | 1.1223 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8417 mL | |
| 100 mM | 0.0269 mL | 0.1347 mL | 0.2694 mL | 0.6734 mL |