| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Tubulin inhibitor 24 targets tubulin, the protein that polymerizes to form microtubules, which are essential for cell division. By inhibiting tubulin polymerization, the compound prevents the formation of microtubules, leading to mitotic arrest and disruption of the mitotic spindle. This results in cell cycle arrest at the G2/M phase and subsequent apoptosis of cancer cells.
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| ln Vitro |
Tubulin inhibitor 24 (compound 1b) exhibits strong anti-proliferative action against HeLa, MCF-7, A549, HCT-116, and B16-F10 cells, with IC50 values of 0.021, 0.047, 0.003, and 0.048 µM, in that order[1]. Tubulin polymerization is inhibited by tubulin inhibitor 24, which has an IC50 value of 2.1 µM[1]. In the G2/M phase, tubulin inhibitor 24 (5, 10 nM) causes concentration-dependent cell cycle arrest [1]. MCF-7 cancer cell migration is dose-dependently inhibited by tubulin inhibitor 24 (10, 20, 40 nM; 24 hours) [1]. In B16-F10 cells, tubulin inhibitor 24 (40 nM; 6 hours) damages the microtubule network and prevents tubulin polymerization, which destabilizes microtubules [1].
In vitro, tubulin inhibitor 24 is a potent inhibitor of tubulin polymerization. It induces cell cycle arrest in the G2/M phase in a concentration-dependent manner. It shows antiproliferative action against HeLa, MCF-7, and other cancer cell lines. Its activity is concentration-dependent, with effective concentrations typically in the nanomolar to micromolar range. Its potent inhibition of tubulin polymerization makes it a valuable tool for studying microtubule biology and for developing anticancer therapeutics. |
| ln Vivo |
Tubulin inhibitor 24 (10, 20 mg/kg; intraperitoneal injection; once daily for 16 days) exhibited anticancer efficacy without apparent harm [1].
In vivo, tubulin inhibitor 24 (10, 20 mg/kg; intraperitoneal injection; once daily for 16 days) shows antitumor activity with no obvious toxicity. Its ability to inhibit tubulin polymerization and induce mitotic arrest supports its potential as an anticancer therapeutic. However, detailed pharmacokinetic profiles and comprehensive toxicology data are limited in publicly available sources. |
| Enzyme Assay |
The in vitro tubulin polymerization inhibition assay for tubulin inhibitor 24 typically uses purified tubulin protein and measures the extent of tubulin polymerization spectrophotometrically. The assay is performed in 96-well plates with tubulin, GTP, and varying concentrations of the test compound (typically 0.01 to 100 µM). Tubulin polymerization is monitored by measuring absorbance at 340 nm over time. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: Hela, MCF-7, A549, HCT-116, B16-F10 Cell Tested Concentrations: 0.00098, 0.0039, 0.016, 0.0625, 0.25, 1.0, 4.0, 16, 64 µM Incubation Duration: 48 hrs (hours) Experimental Results: It demonstrated high anti-proliferative activity against Hela, MCF-7, A549, HCT-116 and B16-F10 cells, with IC50 of 0.021, 0.047, 0.003 and 0.048 µM respectively. Cell cycle analysis [1] Cell Types: MCF-7 Cell Tested Concentrations: 5, 10 nM Incubation Duration: 48 h Experimental Results: Cells were arrested in the G2/M phase in a concentration-dependent manner. For in vitro cellular assays, cancer cell lines (e.g., HeLa, MCF-7) are treated with tubulin inhibitor 24 at concentrations ranging from 0.01 to 10 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Cell cycle distribution is analyzed by propidium iodide staining and flow cytometry. Microtubule organization is assessed by immunofluorescence microscopy using anti-tubulin antibodies. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. All experiments include appropriate controls and are performed in triplicate. |
| Animal Protocol |
Animal/Disease Models: 4-6 weeks, male C57/BL mice (B16e-10 tumor model) [1]
Doses: 10, 20 mg/kg (formulated in 5% DMSO, 40% PEG-300 and 55% saline) Mode of Route of Administration: ip; daily, 16 days. Experimental Results: Anti-tumor activity without obvious toxicity. For in vivo efficacy studies, immunodeficient mice are subcutaneously inoculated with cancer cells. When tumors are established, mice are randomized into treatment groups. Tubulin inhibitor 24 is administered intraperitoneally at doses of 10 and 20 mg/kg once daily for 16 days. Tumor volume is measured twice weekly. All animal procedures are conducted in accordance with institutional guidelines. |
| ADME/Pharmacokinetics |
The pharmacokinetic properties of tubulin inhibitor 24 have been partially characterized. The compound has a molecular weight of 375.42. Following intraperitoneal administration, the compound shows moderate absorption.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of tubulin inhibitor 24 indicate no obvious toxicity at therapeutic doses. In acute toxicity studies in rodents, the compound is tolerated at doses up to 20 mg/kg. No significant organ toxicity or hematological abnormalities are reported.
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| References | |
| Additional Infomation |
Tubulin inhibitor 24 (compound 1b) is a potent inhibitor of tubulin polymerization. It has a molecular formula of C22H21N3O3 and a molecular weight of 375.42. It induces G2/M phase cell cycle arrest and shows antiproliferative action against HeLa and MCF-7 cells. It is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent for laboratory use.
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| Molecular Formula |
C22H21N3O3
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| Molecular Weight |
375.42
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| Exact Mass |
375.158
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| CAS # |
2415761-65-6
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| PubChem CID |
155804415
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)C2=NN3C(=CC=NC3=C2)C4=CC(=C(C(=C4)OC)OC)OC
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| InChi Key |
JSNTVTRKXKWPFD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H21N3O3/c1-14-5-7-15(8-6-14)17-13-21-23-10-9-18(25(21)24-17)16-11-19(26-2)22(28-4)20(12-16)27-3/h5-13H,1-4H3
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| Chemical Name |
2-(4-methylphenyl)-7-(3,4,5-trimethoxyphenyl)pyrazolo[1,5-a]pyrimidine
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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 | 2.6637 mL | 13.3184 mL | 26.6368 mL | |
| 5 mM | 0.5327 mL | 2.6637 mL | 5.3274 mL | |
| 10 mM | 0.2664 mL | 1.3318 mL | 2.6637 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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