| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
tubulin polymerization (IC50 = 0.87 μM)
Tubulin inhibitor 6 targets tubulin, the protein that polymerizes to form microtubules. Microtubules are dynamic cytoskeletal structures that play a critical role in various cellular processes, including cell division, intracellular transport, and cell shape maintenance. During mitosis, microtubules form the mitotic spindle, which is responsible for segregating chromosomes into daughter cells. Tubulin inhibitors bind to tubulin and prevent its polymerization into microtubules, thereby disrupting the mitotic spindle and arresting cells in the cell cycle. This leads to cell cycle arrest and ultimately apoptosis. Tubulin inhibitor 6 is a potent inhibitor of tubulin polymerization, with an IC₅₀ of 0.87 μM. Its ability to inhibit tubulin polymerization is the basis for its antiproliferative activity against cancer cells. The compound is a member of the phenothiazine class. |
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| ln Vitro |
Tubulin inhibitor 6 exhibits antiproliferative activity at submicromolar levels[1].
In vitro, Tubulin inhibitor 6 inhibits tubulin polymerization with an IC₅₀ of 0.87 μM. It inhibits the growth of K562 leukemia cells with an IC₅₀ of 840 nM. The compound exhibits antiproliferative activity at submicromolar levels against multiple cancer cell lines. It is a novel and potent tubulin inhibitor with anticancer activity. The compound's activity is dose-dependent, and its effects on cell proliferation can be measured using cell viability assays. The compound's ability to inhibit tubulin polymerization is the basis for its antiproliferative activity. The compound is a member of the phenothiazine class. |
| ln Vivo |
Detailed in vivo activity data for Tubulin inhibitor 6 is not extensively reported in the available literature. However, its potent in vitro antiproliferative activity against cancer cell lines suggests that it may have potential as an anticancer agent in vivo. Typically, the in vivo efficacy of tubulin inhibitors is evaluated in xenograft mouse models. In such a study, immunodeficient mice are implanted with cancer cells, such as K562 cells. When tumors reach a certain size, Tubulin inhibitor 6 is administered orally or intraperitoneally at various doses. Tumor volume is measured regularly, and final tumor weights are recorded. The compound's ability to inhibit tumor growth is assessed by comparing tumor volumes and weights between treated and control groups. The compound's in vivo activity would depend on its pharmacokinetic properties, such as oral bioavailability and tissue distribution. Further studies are needed to fully evaluate the compound's in vivo anticancer activity.
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| Enzyme Assay |
The inhibition of tubulin polymerization by Tubulin inhibitor 6 is typically measured using a spectrophotometric assay. The assay is performed in a 96-well plate format. Tubulin is purified from bovine brain or obtained from a commercial source. The assay mixture contains 100 mM PIPES buffer (pH 6.9), 1 mM GTP, 1 mM MgCl₂, 10% glycerol, and varying concentrations of the test compound. The reaction is initiated by the addition of tubulin. The polymerization of tubulin into microtubules is monitored by measuring the increase in absorbance at 340 nm, which is proportional to the turbidity of the microtubule solution. The increase in absorbance is monitored over time using a microplate reader. The percentage of inhibition of tubulin polymerization at each compound concentration is calculated relative to a control without inhibitor. The IC₅₀, representing the concentration that inhibits polymerization by 50%, is determined from the dose-response curve. This assay provides a direct measure of the compound's ability to inhibit tubulin polymerization.
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| Cell Assay |
For in vitro cellular assays, the antiproliferative activity of Tubulin inhibitor 6 is typically assessed using various cancer cell lines, such as K562. Cells are seeded in 96-well plates at a density of approximately 5 × 10³ cells per well and allowed to attach overnight. The cells are then treated with Tubulin inhibitor 6 at various concentrations (e.g., 0.1-10 μM) for 48-72 hours. Cell viability is assessed using an MTT or resazurin assay. In the MTT assay, viable cells with active mitochondria reduce MTT to a purple formazan product, which is solubilized and measured spectrophotometrically. The absorbance is directly proportional to the number of viable cells. The percentage of cell viability at each compound concentration is calculated relative to untreated control cells. The IC₅₀, representing the concentration that reduces cell viability by 50%, is determined from the dose-response curve. Cell cycle analysis can be performed by flow cytometry using propidium iodide staining.
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| Animal Protocol |
For in vivo efficacy studies, a xenograft mouse model is commonly employed. Six- to eight-week-old female athymic nude mice are injected subcutaneously in the flank with 5 × 10⁶ K562 cancer cells suspended in Matrigel. When tumors reach a volume of approximately 100-150 mm³, the mice are randomized into treatment groups (n=6-8 per group). Tubulin inhibitor 6 is formulated in a suitable vehicle, such as a solution in DMSO/PEG300/Tween-80/saline. The compound is administered orally or intraperitoneally at various doses (e.g., 1, 5, 10 mg/kg) once daily or every other day for a period of 2-3 weeks. A control group receives the vehicle alone. Tumor volume is measured every 2-3 days using calipers, and body weight is recorded. At the end of the study, the mice are euthanized, and tumors are excised and weighed. The efficacy of the compound is evaluated by comparing tumor growth curves and final tumor weights between treated and control groups. Tumor tissues may be collected for histological analysis and biomarker studies to assess the compound's effects on tubulin polymerization and cell cycle progression.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties for Tubulin inhibitor 6 are not extensively reported in the available literature. The compound has a molecular weight of 367.85 and is soluble in DMSO (20-62.5 mg/mL) and ethanol (~5 mg/mL). It is formulated for in vivo administration using a combination of DMSO and corn oil. Specific pharmacokinetic parameters such as half-life, volume of distribution, clearance, and oral bioavailability have not been determined experimentally. The compound's metabolism is likely to involve hepatic cytochrome P450 enzymes. The compound's elimination route is unknown. Further studies are needed to fully characterize the pharmacokinetic profile of this compound. The compound's in vivo activity would depend on its ability to reach target tissues in sufficient concentrations.
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| Toxicity/Toxicokinetics |
Toxicological data for Tubulin inhibitor 6 is limited, as it is a research chemical. Standard safety precautions should be observed when handling this compound. No specific toxicity studies, such as acute or chronic toxicity in animal models, have been detailed in the public domain. As a tubulin inhibitor, the compound is expected to have antiproliferative effects on rapidly dividing cells, which could lead to side effects such as myelosuppression and gastrointestinal toxicity. However, these have not been assessed. The compound is not approved for clinical use and should only be used in preclinical research settings.
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| References | |
| Additional Infomation |
Tubulin inhibitor 6 is a research tool for studying the role of microtubules in cell division and for developing new anticancer therapies. Its mechanism of action involves inhibition of tubulin polymerization. It has an IC₅₀ of 0.87 μM for tubulin polymerization. It is not approved for clinical use.
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| Molecular Formula |
C20H14NO2SCL
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|---|---|
| Molecular Weight |
367.84866
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| Exact Mass |
367.04
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| Elemental Analysis |
C, 65.30; H, 3.84; Cl, 9.64; N, 3.81; O, 8.70; S, 8.72
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| CAS # |
105925-39-1
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| Related CAS # |
105925-39-1
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| PubChem CID |
2359994
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| Appearance |
White to off-white solid powder
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| LogP |
5.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
482
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
CSWHYHPUEDNIQY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H14ClNO2S/c1-24-15-9-6-13(7-10-15)20(23)22-16-4-2-3-5-18(16)25-19-11-8-14(21)12-17(19)22/h2-12H,1H3
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| Chemical Name |
(2-chlorophenothiazin-10-yl)-(4-methoxyphenyl)methanone
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| Synonyms |
Tubulin inhibitor 6; iHAP1; CUN25391; CUN 25391; CUN-25391
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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: 20~62.5 mg/mL (54.4~169.9 mM)
Ethanol: ~5 mg/mL (~13.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (16.99 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 62.5 mg/mL clear DMSO stock solution to 900 μL 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 | 2.7185 mL | 13.5925 mL | 27.1850 mL | |
| 5 mM | 0.5437 mL | 2.7185 mL | 5.4370 mL | |
| 10 mM | 0.2718 mL | 1.3592 mL | 2.7185 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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