| Size | Price | Stock | Qty |
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| 100mg |
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| 500mg |
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| 1g | |||
| Other Sizes |
| Targets |
Tubulin inhibitor 35 targets tubulin, the protein that polymerizes to form microtubules. Microtubules are essential components of the cytoskeleton and play critical roles in cell division, intracellular transport, and cellular morphology. By binding to tubulin, the compound inhibits microtubule polymerization and disrupts the mitotic spindle, leading to cell cycle arrest at the G2/M phase and subsequent apoptosis.
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| ln Vitro |
In cell-free biochemical assays, Tubulin inhibitor 35 inhibits tubulin polymerization. The compound prevents the polymerization of purified tubulin into microtubules. This activity is typically measured using turbidimetric assays that monitor the increase in absorbance as tubulin polymerizes into microtubules. The IC50 for inhibition of tubulin polymerization is determined from dose-response curves.
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| ln Vivo |
In cell-based assays, Tubulin inhibitor 35 exhibits anti-proliferative activity against cancer cell lines. The compound disrupts the cellular microtubule network and induces mitotic arrest. Cells treated with the compound accumulate at the G2/M phase of the cell cycle and undergo apoptosis. The compound's effects on cell proliferation, cell cycle distribution, and apoptosis are evaluated in various cancer cell lines.
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| Enzyme Assay |
The cell-free tubulin polymerization assay involves incubation of purified tubulin with the compound at various concentrations in assembly buffer containing GTP. The reaction is incubated at 37°C, and microtubule polymerization is monitored by measuring absorbance at 340 nm. The inhibition of tubulin polymerization is determined from dose-response curves. The compound's binding site on tubulin can be studied using competitive binding assays with known tubulin-binding agents.
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| Cell Assay |
Cell-based assays for Tubulin inhibitor 35 involve culturing cancer cell lines and treating them with the compound at concentrations ranging from 0.001 to 10 μM. Cells are incubated for 24-72 hours, and cell viability is assessed using MTT or CCK-8 assays. Cell cycle analysis is performed by flow cytometry. The effect on the microtubule network is assessed by immunofluorescence staining of tubulin. Apoptosis is evaluated by Annexin V staining or caspase activity assays.
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| Animal Protocol |
In animal models, Tubulin inhibitor 35 has been evaluated for its anti-tumor activity. Typical studies involve administration of the compound to tumor-bearing mice via intraperitoneal or intravenous routes at doses determined from toxicity studies. Tumor volumes are measured, and tissues are collected for analysis of tubulin polymerization inhibition, mitotic arrest, and apoptosis. Efficacy is assessed by tumor growth inhibition and survival延长.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Tubulin inhibitor 35 have not been extensively reported. As a small molecule tubulin inhibitor, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound's pharmacokinetic properties depend on its specific chemical structure. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
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| Toxicity/Toxicokinetics |
Tubulin inhibitor 35 is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this chemical reagent. As a tubulin inhibitor, the compound may have toxicity toward rapidly dividing cells, which could translate to bone marrow suppression and gastrointestinal toxicity. Standard toxicity studies would be required for therapeutic development.
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| References |
[1]. Deng J, et al. N(14)-substituted evodiamine derivatives as dual topoisomerase 1/tubulin-Inhibiting anti-gastrointestinal tumor agents. Eur J Med Chem. 2023 Jul 5;255:115366.
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| Additional Infomation |
Tubulin inhibitor 35 is a research-grade compound supplied for cancer research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a tubulin polymerization inhibitor with potential anticancer activity. This product is intended for research use only.
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| Molecular Formula |
C21H21N3O
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|---|---|
| Molecular Weight |
331.410944700241
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| Exact Mass |
331.17
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| Elemental Analysis |
C, 76.11; H, 6.39; N, 12.68; O, 4.83
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| CAS # |
2247047-77-2
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| PubChem CID |
168476159
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
523
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C2C3=C(CCN2C(=O)C4=CC=CC=C41)C5=CC=CC=C5N3
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| InChi Key |
JSGWJWGKFPBVTK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H21N3O/c1-2-12-23-18-10-6-4-8-16(18)21(25)24-13-11-15-14-7-3-5-9-17(14)22-19(15)20(23)24/h3-10,20,22H,2,11-13H2,1H3
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| Chemical Name |
14-propyl-8,13,13b,14-tetrahydroindolo[2',3':3,4]pyrido[2,1-b]quinazolin-5(7H)-one
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| Synonyms |
Tubulin inhibitor 35; Tubulin inhibitor-35; Tubulin inhibitor35
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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 | 3.0174 mL | 15.0871 mL | 30.1741 mL | |
| 5 mM | 0.6035 mL | 3.0174 mL | 6.0348 mL | |
| 10 mM | 0.3017 mL | 1.5087 mL | 3.0174 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.
Products are for research use only; We do not sell to patients
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