| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Targets |
Rosabulin targets tubulin, the protein that polymerizes to form microtubules. It binds to tubulin in a similar manner as colchicine. By binding to tubulin, rosabulin inhibits microtubule assembly, disrupting the mitotic spindle and leading to cell cycle arrest and apoptosis. This mechanism classifies it as a microtubule inhibitor and vascular-disrupting agent.
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| ln Vitro |
Rosabulin (STA 5312) has IC50 values that reach the nanomolar range and demonstrates strong in vitro antiproliferative activity against a range of cancer cell lines, including blood and solid tumor cell lines of different sources (e.g., leukemia, lymphoma, breast cancer, colon cancer, and uterine cancer). Rosabulin also has a non-drug-resistant (MDR) phenotype on cell lines. Rosabulin acts by preventing the assembly of microtubules, which stops the cell cycle [1].
Rosabulin inhibits microtubule assembly in vitro. It binds to tubulin in a similar manner as colchicine. As a vascular-disrupting agent, it disrupts tumor vasculature and suppresses tumor cell proliferation. Its broad-spectrum anti-tumor activity has been demonstrated in preclinical studies. |
| ln Vivo |
Rosabulin (STA 5312) when given orally or intravenously exhibits in vivo action in a range of mice malignancies as well as human tumor xenograft models, including drug-resistant tumors [1].
Rosabulin is an orally active compound with broad-spectrum anti-tumor activity in vivo. As a vascular-disrupting agent, it disrupts tumor vasculature, leading to tumor necrosis and suppression of tumor cell proliferation. It has been evaluated in preclinical models of various cancers, showing potential as an anticancer therapeutic. |
| Enzyme Assay |
The in vitro activity of Rosabulin is assessed using tubulin polymerization assays. In these assays, purified tubulin is incubated with the compound, and the extent of microtubule assembly is measured spectrophotometrically. The compound's ability to inhibit tubulin polymerization is assessed, and IC50 values are calculated.
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| Cell Assay |
Cell-based assays are used to evaluate Rosabulin's antiproliferative activity. Various cancer cell lines are treated with Rosabulin at various concentrations, and cell viability is measured using MTT, XTT, or CellTiter-Glo assays after 48-72 hours of treatment. The compound's ability to disrupt the mitotic spindle can be assessed by immunofluorescence staining of tubulin. IC50 values for proliferation inhibition are calculated.
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| Animal Protocol |
Rosabulin has been evaluated in murine xenograft models of various cancers. In these studies, the compound is typically administered orally to tumor-bearing mice. Tumor volumes are measured twice weekly, and body weight is monitored for toxicity. The compound's ability to inhibit tumor growth and disrupt tumor vasculature is assessed.
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| ADME/Pharmacokinetics |
Rosabulin has a molecular weight of 400.45 and a molecular formula of C22H16N4O2S. Its chemical name is 3-[(4-Cyanophenyl)methyl]-N-(3-methyl-5-isothiazolyl)-alpha-oxo-1-indolizineacetamide. It is an orally active microtubule inhibitor. Purity is typically >98%. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
Rosabulin is a research compound and its full toxicological profile is not detailed in the available literature. As a microtubule inhibitor and vascular-disrupting agent, it has the potential for significant toxicity, particularly on rapidly dividing cells and endothelial cells. Its safety profile would be evaluated in preclinical toxicology studies for its development as a therapeutic agent.
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| References | |
| Additional Infomation |
Roxabulin is a small-molecule angiogenic agent with potential antimitotic and antitumor activities. Similar to colchicine, roxabulin binds to tubulin and inhibits microtubule assembly. This leads to disruption of the cytoskeleton of tumor endothelial cells, ultimately resulting in cell cycle arrest and cell division arrest. By disrupting proliferating vascular cells, tumor blood flow is reduced, ultimately leading to decreased tumor cell proliferation.
Rosabulin (CAS#: 501948-05-6) is a potent and orally active microtubule inhibitor, also known as STA 5312. It binds to tubulin in a similar manner as colchicine and inhibits microtubule assembly. As a vascular-disrupting agent, it disrupts tumor vasculature and suppresses tumor cell proliferation. Rosabulin has broad-spectrum anti-tumor activity and is a valuable research tool for studying microtubule biology and cancer therapy. |
| Molecular Formula |
C22H16N4O2S
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|---|---|
| Molecular Weight |
400.45304
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| Exact Mass |
400.099
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| CAS # |
501948-05-6
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| PubChem CID |
9843935
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.34
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| Melting Point |
233ºC
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| Index of Refraction |
1.7
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| LogP |
4.061
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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 |
5
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| Heavy Atom Count |
29
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| Complexity |
669
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IZZYUABKZYIINT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H16N4O2S/c1-14-10-20(29-25-14)24-22(28)21(27)18-12-17(26-9-3-2-4-19(18)26)11-15-5-7-16(13-23)8-6-15/h2-10,12H,11H2,1H3,(H,24,28)
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| Chemical Name |
2-[3-[(4-cyanophenyl)methyl]indolizin-1-yl]-N-(3-methyl-1,2-thiazol-5-yl)-2-oxoacetamide
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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 : ~50 mg/mL (~124.86 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 | 2.4972 mL | 12.4860 mL | 24.9719 mL | |
| 5 mM | 0.4994 mL | 2.4972 mL | 4.9944 mL | |
| 10 mM | 0.2497 mL | 1.2486 mL | 2.4972 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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