| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
Entasobulin targets β-tubulin and inhibits its polymerization. By binding to tubulin, it disrupts the formation of microtubules, which are essential for cell division, intracellular transport, and maintenance of cell shape. This disruption leads to mitotic arrest and ultimately cell death. Its ability to overcome multidrug resistance (MDR) phenotypes suggests it may not be a substrate for common efflux pumps.
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| ln Vitro |
Entabulin is a small chemical based on indolizide and glyoxalamide that, when tested in vitro, significantly inhibits the proliferation of cancer cell lines, including those with multidrug resistance (MDR) characteristics.
In vitro, entasobulin is an inhibitor of β-tubulin polymerization with substantial anti-proliferative activities against cancer cell lines, including those with multidrug resistance (MDR) phenotypes. As an indolizine glyoxalamide-based small molecule, it demonstrates that it can effectively inhibit the growth of cancer cells, including those that are resistant to other chemotherapeutic agents. |
| ln Vivo |
In vivo, entasobulin has potential anticancer activity. Its activity has been demonstrated in preclinical models. The compound's ability to overcome MDR phenotypes suggests it could be effective in treating cancers that have developed resistance to standard chemotherapies.
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| Enzyme Assay |
Non-cellular assays for entasobulin involve assessing its inhibition of tubulin polymerization using purified tubulin protein. Tubulin is incubated with GTP in the presence of varying concentrations of entasobulin, and the extent of polymerization is measured spectrophotometrically by monitoring the increase in turbidity at 340 nm. The IC₅₀ for inhibition of tubulin polymerization is determined from the dose-response curves.
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| Cell Assay |
In vitro cellular assays for entasobulin involve treating a panel of cancer cell lines, including multidrug-resistant (MDR) lines, with the compound and assessing cell viability and proliferation. Cells are exposed to varying concentrations of entasobulin for 72 hours, and cell viability is measured using MTT or CellTiter-Glo® assays. The IC₅₀ values for growth inhibition are determined from dose-response curves. Cell cycle analysis is performed to assess mitotic arrest.
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| Animal Protocol |
In vivo animal experiments with entasobulin are conducted in mouse xenograft models of human cancers. Tumor-bearing mice are treated with entasobulin, and tumor growth inhibition is monitored. The compound's ability to overcome MDR phenotypes is assessed using tumors that are resistant to standard chemotherapies. Standard endpoints include tumor volume measurements, assessment of toxicity, and survival analysis.
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| ADME/Pharmacokinetics |
Entasobulin has a molecular weight of 439.89 and a molecular formula of C₂₆H₁₈ClN₃O₂. It is a solid powder with a purity of ≥98%. The compound is typically stored at -20°C, protected from light and moisture. It is soluble in DMSO. Its IUPAC name is 2-[1-[(4-chlorophenyl)methyl]indol-3-yl]-2-oxo-N-quinolin-6-ylacetamide.
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| Toxicity/Toxicokinetics |
Entasobulin is a research compound for laboratory use only and is not approved for human therapeutic use. In preclinical studies, it has been generally well-tolerated at therapeutic doses. As a β-tubulin polymerization inhibitor, it may cause side effects similar to other microtubule-targeting agents, such as neurotoxicity and myelosuppression. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
James DA, Koya K, Li H, Liang G, Xia Z, Ying W, Wu Y, Sun L. Indole- and indolizine-glyoxylamides displaying cytotoxicity against multidrug resistant cancer cell lines. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1784-7. doi: 10.1016/j.bmcl.2008.02.029. Epub 2008 Feb 16. PubMed PMID: 18308566.
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| Additional Infomation |
Entasobulin (CAS 501921-61-5) is an indolizine-glyoxylamide based small molecule that functions as an inhibitor of β-tubulin polymerization. It has potential anticancer activity and demonstrates substantial in vitro anti-proliferative activities against cancer cell lines, including multidrug resistance (MDR) phenotypes. It is available from various commercial suppliers for research applications.
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| Molecular Formula |
C26H18CLN3O2
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|---|---|
| Molecular Weight |
439.89
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| Exact Mass |
439.108
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| CAS # |
501921-61-5
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| Related CAS # |
501921-61-5;
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| PubChem CID |
10203597
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Index of Refraction |
1.683
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| LogP |
5.36
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
32
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LJIUXAHLYIPHOK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H18ClN3O2/c27-19-9-7-17(8-10-19)15-30-16-22(21-5-1-2-6-24(21)30)25(31)26(32)29-20-11-12-23-18(14-20)4-3-13-28-23/h1-14,16H,15H2,(H,29,32)
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| Chemical Name |
2-(1-(4-chlorobenzyl)-1H-indol-3-yl)-2-oxo-N-(quinolin-6-yl)acetamide.
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| Synonyms |
Entasobulin UNIITB77GU6BFO. Pubchem SID 175427608.
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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 : ~155 mg/mL (~352.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (5.87 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2733 mL | 11.3665 mL | 22.7330 mL | |
| 5 mM | 0.4547 mL | 2.2733 mL | 4.5466 mL | |
| 10 mM | 0.2273 mL | 1.1366 mL | 2.2733 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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