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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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Purity: ≥98%
Edicotinib (formerly known as JNJ-527; JNJ-40346527) is a novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase with anticancer activity. It functions to prevent macrophage survival, proliferation, and differentiation in patients receiving disease-modifying antirheumatic drug (DMARD) therapy but still having active rheumatoid arthritis (RA). Clinical research is being done on this topic. Increased levels of CSF-1 and decreased CD16+ monocytes in JNJ-40346527-treated patients, but not in placebo-treated patients, demonstrated effective target engagement and proof of activity.Pharmacokinetic exposure to JNJ-40346527 and its active metabolites was above the projected concentration needed for pharmacologic activity. A total of 37 patients (58.7%) treated with JNJ-40346527 and 16 (50.0%) treated with placebo reported ≥ 1 adverse event (AE); 1 patient (1.6%) treated with JNJ-40346527 and 3 patients (9.4%) treated with placebo reported ≥ 1 serious AE.
Targets |
CSF-1R (IC50 = 3.2 nM); KIT (IC50 = 20 nM); FLT3 (IC50 = 190 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
The novel selective and orally bioavailable inhibitor of colony-stimulating factor-1 (CSF-1) receptor kinase, edicotinib (previously known as JNJ-40346527), was discovered.
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Cell Assay |
Cell Line: N13 microglial cells
Concentration: 0.1 nM, 1 nM, 10 nM, 100 nM, 1000 nM Incubation Time: 24 hours Result: Prevented CSF1R and ERK1/2 phosphorylation in N13 microglial cells |
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Animal Protocol |
C57BL/6 J (Harlan) mice
3, 10, 30 and 100 mg/kg; 5 days Oral gavage |
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References |
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Molecular Formula |
C27H35N5O2
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Molecular Weight |
461.61
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Exact Mass |
461.28
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Elemental Analysis |
C, 70.25; H, 7.64; N, 15.17; O, 6.93
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CAS # |
1142363-52-7
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Related CAS # |
1559069-92-9 (HCl);1142363-52-7;
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Appearance |
Solid powder
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SMILES |
CC1(CCC(=CC1)C2=C(C=CC(=N2)C3CC(OC(C3)(C)C)(C)C)NC(=O)C4=NC=C(N4)C#N)C
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InChi Key |
BNVPFDRNGHMRJS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H35N5O2/c1-25(2)11-9-17(10-12-25)22-21(32-24(33)23-29-16-19(15-28)30-23)8-7-20(31-22)18-13-26(3,4)34-27(5,6)14-18/h7-9,16,18H,10-14H2,1-6H3,(H,29,30)(H,32,33)
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Chemical Name |
5-cyano-N-[2-(4,4-dimethylcyclohexen-1-yl)-6-(2,2,6,6-tetramethyloxan-4-yl)pyridin-3-yl]-1H-imidazole-2-carboxamide
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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) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.62 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 16.7 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: ≥ 1.67 mg/mL (3.62 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 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 10 mg/mL (21.66 mM) in 17% Polyethylene glycol 12-hydroxystearate in Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1663 mL | 10.8317 mL | 21.6633 mL | |
5 mM | 0.4333 mL | 2.1663 mL | 4.3327 mL | |
10 mM | 0.2166 mL | 1.0832 mL | 2.1663 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 |
NCT03557970 | Terminated | Drug: H3B-6527 Other: Pharmacokinetic Study |
Recurrent Acute Myeloid LeukemiaOHSU Knight Cancer Institute |
October 5, 2018 |
Phase 2 |
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