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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Briciclib (also known as ON 013105; ON 014185) is an orally bioavailable small molecule and a disodium phosphate ester prodrug of ON 013100 with improved water solubility compared to ON 013100. It is a derivative of benzyl styryl sulfone, which may have anticancer properties and suppress the build-up of cyclin D1 in cancer cells. Briciclib binds to eIF4E, preventing the cap-dependent translation of cyclin D1 and other cancer proteins (c-MYC, VEGF), which results in the death of tumor cells, according to in vitro data. In nonclinical tumor models, briciclib has demonstrated potency and activity when paired with multiple chemotherapeutics. In conclusion, data from both in vitro and in vivo studies show that briciclib has the potential to target eIF4E in solid and hematopoietic cancers, and that an oral form of this exciting therapeutic agent may be developed.
Targets |
eIF4
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
Briciclib is a small molecule that prevents cancer cells from accumulating cyclin D1. Cyclin D1 as the target in vitro At nanomolar concentrations (GI50 = 9.8 - 12.2 nM), briciclib inhibits the growth of malignant cell lines of the breast (MCF7 and MDA-MB-231), gastric (AGS), esophageal (OE19, OE33, and FLO-1), and MCL (JEKO-1 and MINO). Cyclin D1, a protein overexpressed in many tumors, is necessary for normal cell cycle progression. The function of the protein known as eukaryotic initiation factor 4E (eIF4E) is necessary for the process known as cap-dependent translation, which regulates the expression of cyclin D1. According to in vitro data, briciclib binds to eIF4E to prevent cyclin D1 and other cancer proteins (c-MYC, VEGF) from being translated cap-dependently, which results in the death of tumor cells. In nonclinical tumor models, briciclib has demonstrated potency and activity when paired with multiple chemotherapeutics.
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Animal Protocol |
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References |
Molecular Formula |
C₁₉H₂₃O₁₀PS
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Molecular Weight |
474.42
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Exact Mass |
474.08
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Elemental Analysis |
C, 48.10; H, 4.89; O, 33.72; P, 6.53; S, 6.76
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CAS # |
865783-99-9
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Related CAS # |
ON-013100;865783-95-5
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Appearance |
Solid powder
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SMILES |
COC1=C(C=C(C=C1)CS(=O)(=O)/C=C/C2=C(C=C(C=C2OC)OC)OC)OP(=O)(O)O
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InChi Key |
LXENKEWVEVKKGV-BQYQJAHWSA-N
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InChi Code |
InChI=1S/C19H23O10PS/c1-25-14-10-17(27-3)15(18(11-14)28-4)7-8-31(23,24)12-13-5-6-16(26-2)19(9-13)29-30(20,21)22/h5-11H,12H2,1-4H3,(H2,20,21,22)/b8-7+
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Chemical Name |
[2-methoxy-5-[[(E)-2-(2,4,6-trimethoxyphenyl)ethenyl]sulfonylmethyl]phenyl] dihydrogen phosphate
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Synonyms |
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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 |
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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) |
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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 | 2.1078 mL | 10.5392 mL | 21.0784 mL | |
5 mM | 0.4216 mL | 2.1078 mL | 4.2157 mL | |
10 mM | 0.2108 mL | 1.0539 mL | 2.1078 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 |
NCT02168725 | Terminated | Drug: briciclib | Neoplasms Advanced Solid Tumor |
Onconova Therapeutics, Inc. | June 2014 | Phase 1 |