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Batabulin is a novel and potent antitumor agent acting as an inhibitor of microtubule polymerization. It binds to beta-tubulin isotypes and is effective against MDR-multidrug-resistant tumors.
| ln Vitro |
Following treatment with BatabuLin (T138067; 30-300 nM; 24 hours; MCF7 cells), cells exhibit a 25–30% tetraploid (4n) DNA content, suggesting that they are planning at the G2/M cell cycle boundary [1]. Treatment with T138067, 30–300 nM, and 24–48 hours on MCF7 cells revealed 25–30% of cells. After 48 hours, 50–80% of the cell population was observed with 100 nM BatabuLin [1]. By specifically and covalently binding to beta-tubulin isoforms, BatabuLin (T138067) prevents microtubule polymerization. At protected Cys-239 shared by the β1, β2, and β4 tubulin isoforms, covalent modification takes place. In BatabuLin, alterations in cell morphology, collapse, and a rise in cell ploidy were observed [1].
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| ln Vivo |
The treatment of drug-sensitive CCRF-CEM tumors with batabuLin (T138067; 40 mg/kg; intraperitoneal injection; once weekly; days 5, 12, and 19; benzothoracic athymic nude mice) suppresses their growth [1].
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| Cell Assay |
Cell Cycle Analysis[1]
Cell Types: MCF7 Cell Tested Concentrations: 30 nM, 100 nM and 300 nM Incubation Duration: 24 hrs (hours) Experimental Results: Shows arrest at G2/M cell cycle boundary. Apoptosis analysis[1] Cell Types: MCF7 Cell Tested Concentrations: 30 nM, 100 nM and 300 nM Incubation Duration: 24 hrs (hours) or 48 hrs (hours) Experimental Results: 25-30% of cells demonstrated diminished DNA content characteristic of apoptotic cells. |
| Animal Protocol |
Animal/Disease Models: Male athymic nude mice (nu/nu) (6-8 weeks old, 20-25 g) were injected with CCRF-CEM cells [1]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; once a week; Day 5, 12 and 19 Experimental Results: Growth of drug-sensitive CCRF-CEM tumors was impaired. |
| References | |
| Additional Infomation |
Batabulin is under investigation in clinical trial NCT00057382 (T138067 Versus Doxorubicin in Chemotherapy-naive, Unresectable, Hepatocellular Carcinoma Patients).
Batabulin is a synthetic pentafluorophenylsulfonamide with potential antineoplastic activity. Batabulin covalently binds to beta tubulin, resulting in a disruption of microtubule polymerization, collapse of the cytoskeleton, cell cycle arrest, and tumor cell apoptosis. |
| Molecular Formula |
C₁₃H₇F₆NO₃S
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|---|---|
| Molecular Weight |
371.26
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| Exact Mass |
371.005
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| CAS # |
195533-53-0
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| Related CAS # |
Batabulin sodium;195533-98-3
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| PubChem CID |
216324
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| Appearance |
White to off-white solid powder
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| Density |
1.629g/cm3
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| Boiling Point |
403.3ºC at 760mmHg
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| Flash Point |
197.7ºC
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| Vapour Pressure |
1.03E-06mmHg at 25°C
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| Index of Refraction |
1.535
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| LogP |
4.484
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
24
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| Complexity |
516
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ROZCIVXTLACYNY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H7F6NO3S/c1-23-7-3-2-5(4-6(7)14)20-24(21,22)13-11(18)9(16)8(15)10(17)12(13)19/h2-4,20H,1H3
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| Chemical Name |
Benzenesulfonamide, 2,3,4,5,6-pentafluoro-N-(3-fluoro-4-methoxyphenyl)-
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| Synonyms |
T 138067 T138067 T-138067 T-67T67 TL 057 Batabulin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~269.35 mM)
Ethanol : ~100 mg/mL (~269.35 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6935 mL | 13.4677 mL | 26.9353 mL | |
| 5 mM | 0.5387 mL | 2.6935 mL | 5.3871 mL | |
| 10 mM | 0.2694 mL | 1.3468 mL | 2.6935 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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