| Size | Price | Stock | Qty |
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| 2mg |
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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 |
Purity: ≥98%
| Targets |
Tubulin polymerization
Crolibulin targets tubulin, specifically the colchicine-binding site on beta-tubulin. It inhibits the polymerization of tubulin into microtubules. By disrupting microtubule dynamics, it causes cell cycle arrest at the G2/M phase and induces apoptosis. |
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| ln Vitro |
Crolibulin exhibits notable cytotoxic activity against HT-29 cells, with an IC50 of 0.52 μM[2].
Crolibulin exhibits strong inhibition of mitosis at the G2/M stage and is effective against a variety of experimental tumors[2]. Crolibulin demonstrates notable cytotoxic effects on HT-29 cells, achieving an IC50 value of 0.52 μM. It is effective against a range of experimental tumors and significantly inhibits mitosis during the G2/M phase. It induces apoptosis and inhibits cell growth. |
| ln Vivo |
Crolibulin has anti-tumor activity. As a vascular disruption agent, it disrupts tumor angiogenesis, resulting in reduced tumor blood flow, tumor hypoxia, and ischemic necrosis. It has potential antineoplastic activity.
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| Enzyme Assay |
Crolibulin is evaluated in cell-free assays for its ability to inhibit tubulin polymerization. The compound is incubated with purified tubulin, and the inhibition of polymerization is measured using spectrophotometric methods. Binding to the colchicine-binding site on beta-tubulin is assessed using competitive binding assays.
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| Cell Assay |
Crolibulin is assessed in cell-based assays using HT-29 cells and other cancer cell lines. Cells are treated with Crolibulin, and cell cycle progression, apoptosis, and cell viability are measured. The compound's effects on microtubule organization are assessed using immunofluorescence microscopy.
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| Animal Protocol |
Crolibulin is administered in animal models to evaluate its antitumor efficacy. It is active against various experimental tumors. Efficacy is assessed by measuring tumor growth inhibition, apoptosis, and tumor blood flow.
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| ADME/Pharmacokinetics |
Crolibulin has a molecular weight of 359.83 and a molecular formula of C17H14BrF3N2O2. It has a CAS number of 1000852-17-4. The compound is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
Crolibulin has cardiovascular toxicity and neurotoxicity. The compound is for research use only and is not intended for human therapeutic use. It has been studied for its potential antineoplastic activity.
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| References |
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| Additional Infomation |
Crolibulin is a novel flavonoid compound. EPC2407 is a novel small molecule angiogenesis disruptor and apoptosis inducer for the treatment of patients with advanced solid tumors and lymphomas. It is indicated for the treatment of patients with highly vascularized advanced solid tumors. These tumors include common lung, gastrointestinal, ovarian, and breast cancers. Crolibulin has been used in investigational clinical trials for the treatment of solid tumors and anaplastic thyroid cancer. Crolibulin is a small molecule microtubule polymerization inhibitor with potential antitumor activity. The microtubule inhibitor EPC2407 binds to the colchicine binding site on β-tubulin, inhibiting microtubule polymerization into microtubules, which may lead to cell cycle arrest, induce apoptosis, and inhibit tumor cell proliferation. As a vasodilation agent (VDA), this drug also disrupts tumor angiogenesis, resulting in reduced tumor blood flow, tumor hypoxia, and ischemic necrosis.
Drug Indications Studied for the treatment of cancer/tumors (not specified). Mechanism of Action This molecule has been shown to induce tumor cell apoptosis and selectively inhibit the growth of proliferating cell lines, including multidrug-resistant cell lines. Crolibulin is also known as EPC2407 and crinobulin. It is a tubulin polymerization inhibitor. It has potential antineoplastic activity. It is not approved for clinical use. |
| Molecular Formula |
C18H17BRN4O3
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|---|---|
| Molecular Weight |
417.26
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| Exact Mass |
416.048
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| Elemental Analysis |
C, 51.81; H, 4.11; Br, 19.15; N, 13.43; O, 11.50
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| CAS # |
1000852-17-4
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| Related CAS # |
1000852-17-4
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| PubChem CID |
23649181
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.711
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
26
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| Complexity |
607
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| Defined Atom Stereocenter Count |
1
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| SMILES |
BrC1C(=C(C([H])=C(C=1[H])[C@@]1([H])C(C#N)=C(N([H])[H])OC2C(=C(C([H])=C([H])C1=2)N([H])[H])N([H])[H])OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
JXONINOYTKKXQQ-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C18H17BrN4O3/c1-24-13-6-8(5-11(19)17(13)25-2)14-9-3-4-12(21)15(22)16(9)26-18(23)10(14)7-20/h3-6,14H,21-23H2,1-2H3/t14-/m1/s1
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| Chemical Name |
(4R)-2,7,8-triamino-4-(3-bromo-4,5-dimethoxyphenyl)-4H-chromene-3-carbonitrile
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| Synonyms |
EPC 2407; EPC-2407; EPC2407; Crolibulin crinobulin
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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: ~125 mg/mL (~299.6 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 | 2.3966 mL | 11.9829 mL | 23.9659 mL | |
| 5 mM | 0.4793 mL | 2.3966 mL | 4.7932 mL | |
| 10 mM | 0.2397 mL | 1.1983 mL | 2.3966 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 |
| NCT01240590 | Completed | Drug: Crolibulin Drug: Cisplatin |
Anaplastic Thyroid Cancer Solid Tumor |
Anaplastic Thyroid Cancer | January 26, 2011 | Phase 1 Phase 2 |
| NCT00423410 | Completed | Drug: EPC2407 (crinobulin) |
Advanced Cancer | EpiCept Corporation | December 2006 | Phase 1 |
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