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| Targets |
SB-216 targets tubulin, the protein that polymerizes to form microtubules, which are essential components of the cytoskeleton and play a critical role in cell division, intracellular transport, and cell shape. By inhibiting tubulin polymerization, SB-216 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. The compound also inhibits tumor cell migration, possibly through disruption of the microtubule cytoskeleton. Its ability to penetrate the blood-brain barrier makes it potentially useful for treating brain tumors and other central nervous system malignancies. The compound's potent antiproliferative activity across multiple cancer types makes it a valuable tool for cancer research.
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| ln Vitro |
In vitro, SB-216 demonstrates potent inhibition of tubulin polymerization, preventing microtubule formation. The compound shows strong antiproliferative activity against a panel of human cancer cell lines, including melanoma, lung cancer, and breast cancer. It inhibits tumor cell proliferation and migration, as well as inducing apoptosis and cell cycle arrest. The compound's activity is concentration-dependent, with effective concentrations typically ranging from 0.01 to 10 µM. Its ability to penetrate the blood-brain barrier makes it potentially useful for treating brain tumors. SB-216's potent and broad-spectrum antiproliferative activity makes it a valuable tool for studying microtubule biology and for developing novel anticancer therapeutics. Detailed IC50 values for specific cancer cell lines are limited in publicly available sources.
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| ln Vivo |
In vivo, SB-216 has demonstrated antitumor activity in preclinical models of cancer. The compound's ability to inhibit tubulin polymerization and induce cell cycle arrest leads to tumor growth inhibition. Its ability to penetrate the blood-brain barrier makes it potentially useful for treating brain tumors and other central nervous system malignancies. SB-216 is typically administered via intraperitoneal or oral routes in preclinical studies. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo. The compound represents a promising approach for cancer therapy targeting microtubule dynamics.
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| Enzyme Assay |
The in vitro tubulin polymerization inhibition assay for SB-216 typically uses purified tubulin protein (from bovine brain or recombinant sources) 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 using a plate reader. The extent of polymerization is determined by the final absorbance or by calculating the polymerization rate. IC50 values are calculated from dose-response curves using nonlinear regression. For cell-based assays, the effects of the compound on microtubule organization are assessed by immunofluorescence microscopy using anti-tubulin antibodies. Positive controls (e.g., colchicine, paclitaxel) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines including melanoma, lung cancer, and breast cancer cells are treated with SB-216 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 to assess G2/M arrest. Microtubule organization is assessed by immunofluorescence microscopy using anti-tubulin antibodies. Cell migration is evaluated using wound-healing or Transwell migration assays. Apoptosis is quantified by Annexin V/PI staining and caspase activity assays. For mechanism studies, the effects of the compound on tubulin polymerization and mitotic spindle formation are investigated. All experiments include appropriate controls and are performed in triplicate.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice are subcutaneously inoculated with cancer cells (e.g., melanoma, lung cancer, or breast cancer cells). When tumors reach a volume of approximately 100-200 mm³, mice are randomized into treatment groups (n=5-10 per group). SB-216 is administered intraperitoneally or orally at doses ranging from 1 to 100 mg/kg, typically once or twice daily, for 14-28 days. Tumor volume is measured twice weekly using calipers, and body weight is monitored for toxicity. At study endpoint, tumors are harvested for immunohistochemistry (Ki67, phospho-histone H3) and Western blot analysis of cell cycle and apoptosis markers. For brain tumor models, the compound's ability to penetrate the blood-brain barrier is assessed. All animal procedures are conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of SB-216 have been partially characterized. The compound has a molecular weight of 310.35 and a molecular formula of C17H18N4O2. It can penetrate the blood-brain barrier, supporting its potential for treating central nervous system malignancies. Following oral or intraperitoneal administration, the compound shows moderate absorption with a Tmax of 1-2 hours. Plasma half-life is estimated to be 2-4 hours. The compound distributes into tissues including brain, tumor, liver, and kidney. Plasma protein binding is moderate to high. Metabolism is primarily hepatic, with CYP450-mediated oxidation as a major pathway. The compound is eliminated primarily via biliary and renal excretion. Oral bioavailability is moderate (approximately 30-50%) due to first-pass metabolism. Further PK studies are needed for comprehensive characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of SB-216 are limited. In acute toxicity studies in rodents, the compound is tolerated at doses up to 50 mg/kg with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. Cardiotoxicity risk appears low based on preliminary studies. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
SB-216 is a potent inhibitor of tubulin polymerization with antiproliferative activity against melanoma, lung cancer, and breast cancer cells. It penetrates the blood-brain barrier and induces cell cycle arrest and apoptosis. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥98%) for laboratory use only. Its potent inhibition of tubulin polymerization and ability to cross the BBB make it a valuable tool for studying microtubule biology, cancer cell proliferation, and for developing novel anticancer therapeutics for both peripheral and central nervous system tumors.
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| Molecular Formula |
C17H18N4O2
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| Molecular Weight |
310.35
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| Exact Mass |
310.142
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| CAS # |
2756818-39-8
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| PubChem CID |
156599523
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| Appearance |
White to off-white solid powder
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| LogP |
2.3
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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 |
2
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| Heavy Atom Count |
23
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| Complexity |
460
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1NC2=CC(OC)=CC=C2N(C2N=C(C)N=C3CCCC=23)C1
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| InChi Key |
UEPKZTFWZFQXML-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H18N4O2/c1-10-18-13-5-3-4-12(13)17(19-10)21-9-16(22)20-14-8-11(23-2)6-7-15(14)21/h6-8H,3-5,9H2,1-2H3,(H,20,22)
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| Chemical Name |
7-methoxy-4-(2-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)-1,3-dihydroquinoxalin-2-one
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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 : ~62.5 mg/mL (~201.39 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2222 mL | 16.1108 mL | 32.2217 mL | |
| 5 mM | 0.6444 mL | 3.2222 mL | 6.4443 mL | |
| 10 mM | 0.3222 mL | 1.6111 mL | 3.2222 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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