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| Targets |
Eg5 Inhibitor V, trans-24 targets the kinesin Eg5 motor protein, binding to the allosteric site of the motor domain and inhibiting its ATPase activity, thereby preventing Eg5 from cross-linking and sliding microtubules, which is essential for proper spindle bipolarity and chromosome segregation during mitosis.
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| ln Vitro |
Research on cancer can benefit from the usage of Eg5 Inhibitor V, trans-24, a strong and selective Eg5 inhibitor with an IC50 of 0.65 μM [1].
In vitro enzymatic assays demonstrate that Eg5 Inhibitor V, trans-24 inhibits Eg5 ATPase activity with an IC50 of 0.65 μM, showing potent and specific inhibition of the kinesin motor protein. |
| ln Vivo |
In vivo, Eg5 Inhibitor V, trans-24 has been studied in cancer models where Eg5 inhibition leads to mitotic arrest, formation of monopolar spindles, and subsequent apoptosis in rapidly dividing tumor cells, supporting its potential as an anticancer therapeutic.
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| Enzyme Assay |
The in vitro enzyme assay for Eg5 inhibition involves incubating Eg5 Inhibitor V, trans-24 with recombinant human Eg5 motor domain, microtubules, and ATP, measuring ATPase activity via malachite green phosphate detection or by monitoring microtubule gliding in motility assays, with IC50 values determined from concentration-response curves.
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| Cell Assay |
In vitro cell culture studies utilize cancer cell lines (e.g., HeLa, MCF-7, A549) treated with Eg5 Inhibitor V, trans-24, assessing cell viability by MTT or CellTiter-Glo, cell cycle analysis by propidium iodide staining and flow cytometry, mitotic spindle morphology by immunofluorescence staining of α-tubulin, and apoptosis detection by Annexin V/PI staining.
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| Animal Protocol |
In vivo animal experiments involve administering Eg5 Inhibitor V, trans-24 to tumor-bearing mice (xenograft models) via intraperitoneal injection or oral gavage, monitoring tumor growth inhibition, performing histopathological analysis of tumors for mitotic index and apoptosis, and assessing survival outcomes in treated versus control groups.
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| ADME/Pharmacokinetics |
Eg5 Inhibitor V, trans-24 has a molecular weight of 423.46 g/mol and is stored as a solid powder at -20°C; it is soluble in DMSO, and solutions should be prepared fresh for in vitro assays, with stability maintained under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological data for Eg5 Inhibitor V, trans-24 are limited to in vitro cytotoxicity assessments; comprehensive in vivo toxicity studies have not been extensively reported, though Eg5 inhibitors as a class can cause myelosuppression and other on-target toxicities due to their effects on proliferating cells.
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| References | |
| Additional Infomation |
Eg5 Inhibitor V, trans-24 is a research compound used for studying mitotic kinesin biology and evaluating the therapeutic potential of Eg5 inhibition in cancer; it has not been approved for clinical use and serves as a valuable tool for investigating the role of Eg5 in cell division and as a lead compound for anticancer drug discovery.
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| Molecular Formula |
C26H21N3O3
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|---|---|
| Molecular Weight |
423.46324
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| Exact Mass |
423.158
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| CAS # |
869304-55-2
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| PubChem CID |
11553595
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| Appearance |
White to light yellow solid powder
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| LogP |
4.227
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
32
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| Complexity |
738
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@H]2C(=O)N(C(=O)N2[C@@H](C3=C1C4=CC=CC=C4N3)C5=CC(=CC=C5)O)CC6=CC=CC=C6
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| InChi Key |
UOKINRKWPYVMSZ-LADGPHEKSA-N
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| InChi Code |
InChI=1S/C26H21N3O3/c30-18-10-6-9-17(13-18)24-23-20(19-11-4-5-12-21(19)27-23)14-22-25(31)28(26(32)29(22)24)15-16-7-2-1-3-8-16/h1-13,22,24,27,30H,14-15H2/t22-,24+/m0/s1
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| Chemical Name |
(10R,15S)-13-benzyl-10-(3-hydroxyphenyl)-8,11,13-triazatetracyclo[7.7.0.02,7.011,15]hexadeca-1(9),2,4,6-tetraene-12,14-dione
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.3615 mL | 11.8075 mL | 23.6150 mL | |
| 5 mM | 0.4723 mL | 2.3615 mL | 4.7230 mL | |
| 10 mM | 0.2361 mL | 1.1807 mL | 2.3615 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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