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Purity: ≥98%
Crolibulin, formerly known as EPC2407 and crinobulin, is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity. The microtubulin inhibitor EPC2407 attaches itself to the beta-tubulin'scolchicine-bindingsite and prevents tubulin from polymerizing into microtubules. This can stop tumor cell growth, induce apoptosis, and stop cell cycle arrest. This agent, which is classified as a vascular disruption agent (VDA), also interferes with the neovascularization of tumors, potentially leading to tumor hypoxia, ischemic necrosis, and decreased tumor blood flow.
| Targets |
Tubulin polymerization
|
|---|---|
| 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]. |
| References |
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| Additional Infomation |
Crolibulin is a neoflavonoid.
EPC2407 is a novel small molecule vascular disruption agent and apoptosis inducer for the treatment of patients with advanced solid tumors and lymphomas. It is intended for the treatment of advanced cancer patients with solid tumors that are well vascularized. These tumors include the frequently occurring cancers of the lung, gastrointestinal tract, ovaries, and breast. Crolibulin has been used in trials studying the treatment of Solid Tumor and Anaplastic Thyroid Cancer. Crolibulin is a small molecule tubulin polymerization inhibitor with potential antineoplastic activity. Microtubulin inhibitor EPC2407 binds to the colchicine-binding site on beta-tubulin and inhibits the polymerization of tubulin into microtubules, which may result in cell cycle arrest, the induction of apoptosis, and the inhibition of tumor cell proliferation. As a vascular disruption agent (VDA), this agent also disrupts tumor neovascularization, which may result in a reduction in tumor blood flow and tumor hypoxia and ischemic necrosis. Drug Indication Investigated for use/treatment in cancer/tumors (unspecified). Mechanism of Action The molecule has been shown to induce tumor cell apoptosis and selectively inhibit growth of proliferating cell lines, including multi-drug resistant cell lines. |
| Molecular Formula |
C18H17BRN4O3
|
|---|---|
| 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
|
| 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
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
26
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| Complexity |
607
|
| Defined Atom Stereocenter Count |
1
|
| 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]
|
| 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
|
| 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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