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Purity: ≥98%
Indibulin is a synthetic small molecule with antimitotic and potential antineoplastic activities. Indibulin destabilizes tubulin polymerization and induces tumor cell cycle arrest and apoptosis by binding to a site on tubulin that is distinct from taxane- or Vinca alkaloid-binding sites. It has been demonstrated that this substance is effective against tumor cell lines that are taxane- and multidrug-resistant (MDR). Use this agent to look up any closed or ongoing clinical trials. (Thesaurus NCI).
| Targets |
Tubulin
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|---|---|
| ln Vitro |
Indibulin (300-2100 nM; 48 hours) has an IC50 of 150 nM, which inhibits the growth of MCF-7 cells.
Indibulin (300, 600 nM; 48 hours) inhibits G2/M phase cells, suggesting that it prevents the cell cycle from progressing during mitosis[1]. Indibulin (150-600 nM; 24 hours) causes MCF-7 cells to undergo apoptosis[1]. When Indibulin (150-600 nM; 48 hours) at concentrations of 300 and 600 nM is used to treat MCF-7 cells, it produces cleaved fragments of the PARP protein[1]. |
| Cell Assay |
Cell Line: MCF-7 cells
Concentration: 300, 600, 900, 1200, 1500, 1800, 2100 nM Incubation Time: 48 hours Result: Inhibited the proliferation of MCF-7 cells with an IC50 of 150 nM. |
| References |
| Molecular Formula |
C22H16CLN3O2
|
|---|---|
| Molecular Weight |
389.83
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| Exact Mass |
389.0931
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| Elemental Analysis |
C, 67.78; H, 4.14; Cl, 9.09; N, 10.78; O, 8.21
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| CAS # |
204205-90-3
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| Related CAS # |
204205-90-3
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| Appearance |
Solid powder
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| SMILES |
C1=CC=C2C(=C1)C(=CN2CC3=CC=C(C=C3)Cl)C(=O)C(=O)NC4=CC=NC=C4
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| InChi Key |
SOLIIYNRSAWTSQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H16ClN3O2/c23-16-7-5-15(6-8-16)13-26-14-19(18-3-1-2-4-20(18)26)21(27)22(28)25-17-9-11-24-12-10-17/h1-12,14H,13H2,(H,24,25,28)
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| Chemical Name |
2-[1-[(4-chlorophenyl)methyl]indol-3-yl]-2-oxo-N-pyridin-4-ylacetamide
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| Synonyms |
ZIO-301; ZINC01996564; ZERO/005632; D-24851; d-24851; NCGC00160428-01
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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: 40~50 mg/mL (102.6~128.3 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (5.34 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.34 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5652 mL | 12.8261 mL | 25.6522 mL | |
| 5 mM | 0.5130 mL | 2.5652 mL | 5.1304 mL | |
| 10 mM | 0.2565 mL | 1.2826 mL | 2.5652 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00591890 | Completed | Drug: indibulin | Advanced Cancer | Alaunos Therapeutics | October 2007 | Phase 1 |
| NCT00591136 | Completed | Drug: indibulin | Solid Tumors | Alaunos Therapeutics | April 2003 | Phase 1 |
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