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Purity: ≥98%
Abrocitinib (formerly known as PF04965842; PF-04965842; Cibinqo) is a novel, potent and orally bioavailable JAK1 (Janus Kinase 1) inhibitor with immunomodulatory and antiinflammatory effects. It inhibits JAK1, JAK2, JAK3 and tyrosine kinase (TYK) 2 with IC50s of 29 nM, 803 nM, > 10 000 nM and 1250 nM, respectively. Abrocitinib is being investigated for treatment of plaque psoriasis. Physicochemical properties and pharmacokinetic parameters of PF-04965842 are examined in rats following doses of 1 mg/kg iv or 3 mg/kg po. Clearance of PF-04965842 is low relative to total liver blood flow (CL = 26.6 mL/min/kg). Vdss = 1.04 L/kg. T1/2 = 1.1 h. The oral availability of PF-04965842 is 95.6%. PF-04965842 demonstrates efficacy in a dose-responsive manner in a therapeutic rat adjuvant-induced arthritis model.
| ln Vitro |
Abrocitinib (compound 25) inhibits, with IC50 values of 189, 163 nM, and 7.178 μM, respectively, the phosphorylation of STAT3 in response to IFNα, the phosphorylation of STAT1 in human whole blood (HWB), and pSTAT5 integrated into CD34+ of HWB (JAK2).
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| ln Vivo |
In a rat adjuvant-induced arthritis model, brachicitinib (Compound 25; 5, 15, 50 mg/kg, orally, once daily for 7 days) significantly decreased paw swelling [1].
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| Animal Protocol |
Animal/Disease Models: Female Lewis rats (8−10 weeks old) [1]
Doses: 5, 15, 50 mg/kg Route of Administration: Oral daily for 7 days Experimental Results: Paw swelling was Dramatically diminished at all doses. |
| References |
[1]. Vazquez ML, et al. Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases. J Med Chem. 2018 Feb 8;61(3):1130-1152.
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| Molecular Formula |
C14H21N5O2S
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| Molecular Weight |
323.41
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| CAS # |
1622902-68-4
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| Related CAS # |
2204280-33-9 (trans-isomer);1622902-68-4 (cis-isomer);
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| SMILES |
CCCS(=O)(N[ C@H]1C[C@@H](N(C)C2=C3C(NC=C3)=NC=N2)C1)=O
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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: ≥ 2.08 mg/mL (6.43 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 20.8 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: ≥ 2.08 mg/mL (6.43 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 20.8 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: ≥ 2.08 mg/mL (6.43 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 | 3.0921 mL | 15.4603 mL | 30.9205 mL | |
| 5 mM | 0.6184 mL | 3.0921 mL | 6.1841 mL | |
| 10 mM | 0.3092 mL | 1.5460 mL | 3.0921 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.
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