| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
After 24 hours of treatment with batabulin (T138067; 30-300 nM; MCF7 cells), cells exhibit 25–30% tetraploid (4n) DNA content, indicating cell cycle arrest at the G2/M cell cycle boundary [1]. 25%–30% of MCF7 cells treated with batabulin (T138067; 30-300 nM; 24-48 hours) underwent apoptosis. Of the cell population, 50–80% are undergoing apoptosis after 48 hours of exposure to 100 nM Batabulin [1]. Microtubule polymerization is disrupted by the selective covalent binding of batabulin (T138067) to a subset of β-tubulin isoforms. At conserved Cys-239, which is shared by tubulin isoforms β1, β2, and β4, covalent modification takes place. Batabulin-exposed cells exhibit increased chromosomal ploidy, cytoskeletal collapse, and morphological changes [1].
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| ln Vivo |
The treatment of male athymic nude mice with batabulin (T138067; 40 mg/kg; i.p.; weekly; days 5, 12, and 19) inhibits the formation of drug-sensitive CCRF-CEM tumors [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 Sodium is the sodium salt form of batabulin, a synthetic pentafluorophenylsulfonamide with potential antineoplastic activity. Batabulin covalently binds to and selectively modifies the beta 1, beta 2, beta 3, and beta 4 isotypes of beta tubulin at a conserved cysteine residue, resulting in disruption of microtubule polymerization, collapse of the cytoskeleton, an increase in chromosomal ploidy, cell cycle arrest, and tumor cell apoptosis.
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| Molecular Formula |
C13H6F6NNAO3S
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|---|---|
| Molecular Weight |
393.23
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| Exact Mass |
392.987
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| CAS # |
195533-98-3
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| Related CAS # |
Batabulin;195533-53-0
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| PubChem CID |
23669770
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| Appearance |
Off-white to light yellow solid powder
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| Boiling Point |
403.3ºC at 760 mmHg
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| Flash Point |
197.7ºC
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| Vapour Pressure |
1.03E-06mmHg at 25°C
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| LogP |
5.004
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
522
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
UWPXRVDIKGZQQW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H6F6NO3S.Na/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;/h2-4H,1H3;/q-1;+1
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| Chemical Name |
sodium;(3-fluoro-4-methoxyphenyl)-(2,3,4,5,6-pentafluorophenyl)sulfonylazanide
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| Synonyms |
T138067 T-138067 Batabulin sodium BatabulinT 138067
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 : ~125 mg/mL (~317.87 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5430 mL | 12.7152 mL | 25.4304 mL | |
| 5 mM | 0.5086 mL | 2.5430 mL | 5.0861 mL | |
| 10 mM | 0.2543 mL | 1.2715 mL | 2.5430 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00003359 | COMPLETED | Drug: batabulin sodium | Unspecified Adult Solid Tumor, Protocol Specific | Memorial Sloan Kettering Cancer Center | 1998-04 | Phase 1 |
| NCT00022243 | UNKNOWN STATUS | Drug: batabulin sodium | Lung Cancer | Tularik | 2000-10 | Phase 2 |
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