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| Targets |
Antiproliferative agent-14 targets tubulin polymerization. By inhibiting tubulin polymerization, it disrupts microtubule dynamics, which is essential for mitotic spindle formation and cell division. The compound also inhibits colchicine binding activity. Its mechanism involves disrupting critical signaling pathways controlling the cell cycle.
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| ln Vitro |
Compound 3b, also known as antiproliferative agent-14, exhibits antiproliferative action against HeLa cells (IC50=13 nM)[1]. Colchicine binding activity is inhibited by antiproliferative agent-14, with a 72.2% inhibitory percentage[1].
In vitro, Antiproliferative agent-14 exhibits antiproliferative action against HeLa cells with an IC50 of 13 nM. It is a potent tubulin polymerization inhibitor with an IC50 of 3.41 μM. The compound inhibits colchicine binding activity with a 72.2% inhibitory percentage. It arrests cells at the G2/M phase of the cell cycle and has excellent antiproliferative activity. |
| ln Vivo |
In vivo, Antiproliferative agent-14 has been shown to inhibit tumor growth in animal models. Its ability to arrest cells at the G2/M phase and inhibit tubulin polymerization makes it a potential candidate for cancer therapy. The compound's antiproliferative activity has been evaluated in xenograft models, although detailed in vivo pharmacokinetic and toxicological data are limited. Further studies are needed to fully characterize its in vivo efficacy and safety.
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| Enzyme Assay |
For non-cellular assays, Antiproliferative agent-14 is evaluated for its ability to inhibit tubulin polymerization. Purified tubulin is incubated with the compound, and polymerization is monitored spectrophotometrically at 340 nm. IC50 values are calculated from dose-response curves. Colchicine binding inhibition is assessed using competitive binding assays with radiolabeled colchicine. The compound's ability to disrupt microtubule dynamics is confirmed using in vitro polymerization assays.
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| Cell Assay |
In vitro cell culture experiments are performed using cancer cell lines including HeLa cells and other proliferating cell lines. Cells are treated with Antiproliferative agent-14 at concentrations ranging from 1 nM to 10 μM for 24-72 hours. Endpoints include cell viability (MTT assay), cell cycle analysis (flow cytometry, G2/M arrest), apoptosis (Annexin V/PI staining), and tubulin polymerization status (immunofluorescence). The compound's antiproliferative activity is confirmed across multiple cell lines.
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| Animal Protocol |
In vivo animal studies are conducted in mouse xenograft models of cancer. Antiproliferative agent-14 is administered intraperitoneally or orally at various doses. Efficacy is assessed by measuring tumor volume, tumor weight, and survival rates. Pharmacodynamic endpoints include cell cycle analysis of tumor tissues, apoptosis markers, and tubulin polymerization status. Pharmacokinetic parameters such as bioavailability, half-life, and tissue distribution are determined to guide dosing regimens.
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| ADME/Pharmacokinetics |
Antiproliferative agent-14 has a molecular formula and weight of approximately 363.38 g/mol. It is a small molecule inhibitor of tubulin polymerization. The compound is typically dissolved in DMSO for in vitro studies and formulated in appropriate vehicles for in vivo administration. Pharmacokinetic properties are not fully characterized, but the compound is expected to have moderate bioavailability based on its chemical properties. It is stable under recommended storage conditions.
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| Toxicity/Toxicokinetics |
Toxicological profiles of Antiproliferative agent-14 are not fully characterized. In vitro cytotoxicity has been observed in cancer cell lines at nanomolar concentrations. The compound's ability to inhibit tubulin polymerization may affect normal proliferating cells, leading to potential toxicity in rapidly dividing tissues. Standard safety precautions should be followed during handling. The compound is for research use only and is not intended for therapeutic applications without further development.
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| References | |
| Additional Infomation |
Antiproliferative agent-14 (compound 3b, MT189) is a potent tubulin polymerization inhibitor with an IC50 of 3.41 μM. It exhibits excellent antiproliferative activity with an IC50 of 13 nM against HeLa cells and arrests cells at the G2/M phase. The compound inhibits colchicine binding activity. It is used in cancer research to study microtubule dynamics and cell cycle regulation. The compound is for research use only and is not approved for clinical use.
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| Molecular Formula |
C21H18FN3O2
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|---|---|
| Molecular Weight |
363.38
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| Exact Mass |
363.138
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| CAS # |
1885900-35-5
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| PubChem CID |
86280647
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
474
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N(C1N2C=C(F)C=CC2=NC=1C1C=CC=CC=1O)CC1C=CC(OC)=CC=1
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| InChi Key |
QBNMSKFVSPKNSV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18FN3O2/c1-27-16-9-6-14(7-10-16)12-23-21-20(17-4-2-3-5-18(17)26)24-19-11-8-15(22)13-25(19)21/h2-11,13,23,26H,12H2,1H3
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| Chemical Name |
2-[6-fluoro-3-[(4-methoxyphenyl)methylamino]imidazo[1,2-a]pyridin-2-yl]phenol
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ≥ 100 mg/mL (275.19 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 | 2.7519 mL | 13.7597 mL | 27.5194 mL | |
| 5 mM | 0.5504 mL | 2.7519 mL | 5.5039 mL | |
| 10 mM | 0.2752 mL | 1.3760 mL | 2.7519 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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