| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Tubulin (colchicine binding site). As a microtubule destabilizer, it binds to β-tubulin at the colchicine site, preventing microtubule polymerization and leading to mitotic arrest. It is a CBSI (colchicine binding site inhibitor).
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| ln Vitro |
ABI-274 significantly enhances cancer cell apoptosis in vitro when used in combination with vemurafenib, exhibiting strong synergistic effects. It has demonstrated potent antiproliferative activity against various cancer cell lines. Detailed IC50 values for specific cell lines are available upon request from suppliers.
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| ln Vivo |
ABI-274 has demonstrated potent anticancer activities in vivo. As an orally bioavailable compound, it shows efficacy in animal models of cancer, with favorable pharmacokinetics contributing to its in vivo activity. Detailed efficacy data in specific xenograft models can be obtained from the primary literature.
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| Enzyme Assay |
In vitro tubulin polymerization assays are performed using purified tubulin protein and assessing the turbidity increase over time at 340 nm. The compound's ability to inhibit polymerization is measured, and IC50 values are calculated. Competitive binding assays with [3H]colchicine are used to confirm binding at the colchicine site.
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| Cell Assay |
Cell viability is assessed using standard assays such as MTT, CCK-8, or CellTiter-Glo in various cancer cell lines. Cells are treated with serial dilutions of ABI-274 for 48-72 hours. Apoptosis is measured by Annexin V/PI staining and flow cytometry. Combination studies with vemurafenib are performed using fixed-ratio dilution methods.
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| Animal Protocol |
In vivo efficacy studies are conducted in mouse xenograft models. ABI-274 is administered orally at various dose levels (e.g., 10, 30, 100 mg/kg) on a daily or intermittent schedule. Tumor growth inhibition is assessed by caliper measurements. Body weight and clinical signs are monitored for toxicity assessment. Tumors are harvested for histology and biomarker analysis.
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| ADME/Pharmacokinetics |
ABI-274 is orally bioavailable with favorable pharmacokinetic properties. It has a molecular weight of 352.38 and a LogP of 4.32. It is typically formulated in DMSO for in vitro studies and can be administered orally in vivo. Detailed PK parameters (Cmax, Tmax, AUC, half-life) are available from specialized pharmacological databases.
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| Toxicity/Toxicokinetics |
Detailed toxicological profiles of ABI-274 are not extensively reported in the literature. As a tubulin inhibitor, it may cause dose-limiting toxicities such as myelosuppression and neurotoxicity, consistent with other agents in this class. In preclinical studies, the compound shows a manageable safety profile at therapeutic doses.
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| References |
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| Additional Infomation |
ABI-274 is a research compound belonging to the CBSI class of tubulin inhibitors. It is being investigated for its potential in cancer therapy, particularly in combination with other agents like vemurafenib. It is not approved for clinical use and is exclusively for research purposes. Its molecular formula is C20H20N2O4 and its molecular weight is 352.38.
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| Molecular Formula |
C20H20N2O4
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|---|---|
| Molecular Weight |
352.384
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| Exact Mass |
352.142
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| CAS # |
1253697-93-6
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| PubChem CID |
49787837
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
587.7±50.0 °C at 760 mmHg
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| Flash Point |
309.2±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.585
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| LogP |
4.32
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
453
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)C2=NC=C(C(=O)C3=CC(=C(C(=C3)OC)OC)OC)N2
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| InChi Key |
NQHVDNDKHQBFKP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H20N2O4/c1-12-5-7-13(8-6-12)20-21-11-15(22-20)18(23)14-9-16(24-2)19(26-4)17(10-14)25-3/h5-11H,1-4H3,(H,21,22)
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| Chemical Name |
[2-(4-methylphenyl)-1H-imidazol-5-yl]-(3,4,5-trimethoxyphenyl)methanone
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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 | 2.8378 mL | 14.1892 mL | 28.3785 mL | |
| 5 mM | 0.5676 mL | 2.8378 mL | 5.6757 mL | |
| 10 mM | 0.2838 mL | 1.4189 mL | 2.8378 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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