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1mg |
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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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100mg |
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250mg |
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Itacitinib adipate, the adipate salt of itacitinib which is also known as INCB39110, is a potent, selective and orally bioavailable inhibitor of JAK1 (Janus-associated kinase 1) with potential antineoplastic activity, currently in Phase II clinical trials for the treatment of myelofibrosis, rheumatoid arthritis and plaque psoriasis.
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ln Vivo |
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Animal Protocol |
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References |
Haematologica.2017 Feb;102(2):327-335;Expert Opin Ther Pat.2017 Feb;27(2):127-143;AACR; Cancer Res. 2015, 75(15 Suppl).
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Molecular Formula |
C₃₂H₃₃F₄N₉O₅
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Molecular Weight |
699.66
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CAS # |
1334302-63-4
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Related CAS # |
Itacitinib;1334298-90-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
N#CCC1(N2N=CC(C3=C4C(NC=C4)=NC=N3)=C2)CN(C5CCN(C(C6=C(F)C(C(F)(F)F)=NC=C6)=O)CC5)C1 .O=C(O)CCCCC(O)=O
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Chemical Name |
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
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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: ≥ 2.5 mg/mL (3.57 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 25.0 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: ≥ 2.5 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (3.57 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4293 mL | 7.1463 mL | 14.2927 mL | |
5 mM | 0.2859 mL | 1.4293 mL | 2.8585 mL | |
10 mM | 0.1429 mL | 0.7146 mL | 1.4293 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 |
NCT04239989 | Recruiting | Drug: Itacitinib Drug: Itacitinib Adipate |
Bronchiolitis Obliterans | M.D. Anderson Cancer Center | April 8, 2021 | Phase 1 |
NCT04070781 | Terminated | Drug: Itacitinib Drug: Tocilizumab | Steroid Refractory GVHD Graft Vs Host Disease |
Columbia University | January 20, 2020 | Phase 1 |
NCT04339101 | Active, not recruiting Has Results |
Drug: Fludarabine Drug: Itacitinib Adipate |
Acute Leukemia Hematologic and Lymphocytic Disorder |
City of Hope Medical Center | November 11, 2020 | Phase 2 |
NCT04200365 | Terminated | Drug: Itacitinib | Chronic Graft-versus-host-disease | SCRI Development Innovations, LLC | June 5, 2020 | Phase 2 |
Treatment effects on total symptom score (TSS).Haematologica.2017 Feb;102(2):327-335 td> |
Treatment effects on spleen volume.Haematologica.2017 Feb;102(2):327-335. td> |
Mean hemoglobin level and platelet count over time by dose cohort.Haematologica.2017 Feb;102(2):327-335. td> |