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PF-03394197(Oclacitinib)

Novel Janus kinase inhibitor CAS# 1208319-26-9

PF-03394197(Oclacitinib)

Catalog No. BCC6474----Order now to get a substantial discount!

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PF-03394197(Oclacitinib): 5mg $161 In Stock
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Quality Control of PF-03394197(Oclacitinib)

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Chemical structure

PF-03394197(Oclacitinib)

3D structure

Chemical Properties of PF-03394197(Oclacitinib)

Cas No. 1208319-26-9 SDF Download SDF
PubChem ID 44631938 Appearance Powder
Formula C15H23N5O2S M.Wt 337.44
Type of Compound N/A Storage Desiccate at -20°C
Solubility >33.7mg/mL in DMSO
Chemical Name N-methyl-1-[4-[methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclohexyl]methanesulfonamide
SMILES CNS(=O)(=O)CC1CCC(CC1)N(C)C2=NC=NC3=C2C=CN3
Standard InChIKey HJWLJNBZVZDLAQ-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H23N5O2S/c1-16-23(21,22)9-11-3-5-12(6-4-11)20(2)15-13-7-8-17-14(13)18-10-19-15/h7-8,10-12,16H,3-6,9H2,1-2H3,(H,17,18,19)
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

PF-03394197(Oclacitinib) Dilution Calculator

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PF-03394197(Oclacitinib) Molarity Calculator

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Preparing Stock Solutions of PF-03394197(Oclacitinib)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.9635 mL 14.8174 mL 29.6349 mL 59.2698 mL 74.0872 mL
5 mM 0.5927 mL 2.9635 mL 5.927 mL 11.854 mL 14.8174 mL
10 mM 0.2963 mL 1.4817 mL 2.9635 mL 5.927 mL 7.4087 mL
50 mM 0.0593 mL 0.2963 mL 0.5927 mL 1.1854 mL 1.4817 mL
100 mM 0.0296 mL 0.1482 mL 0.2963 mL 0.5927 mL 0.7409 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on PF-03394197(Oclacitinib)

Description:

IC50: 10 nM for JAK1

Janus kinase (JAK) enzymes are involved in cell signaling pathways activated by cytokines dysregulated in allergy. PF-03394197 (Oclacitinib) is a novel Janus kinase inhibitor.

In vitro: PF-03394197 inhibited JAK family members by 50% at concentrations ranging from 10 to 99 nM and did not inhibit a panel of 38 non-JAK kinases. PF-03394197 was most potent at inhibiting JAK1. PF-03394197 also inhibited the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. PF-03394197 had minimal effects on cytokines which did not activate the JAK1 enzyme in cells [1].

In vivo: PF-03394197 administered orally at a dose of 0.4–0.6 mg/kg twice daily was safe and efficacious in controlling the pruritus associated with allergic dermatitis. PF-03394197 provided itch relief within 24 h that persisted through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7 [2].

Clinical trial: PF-03394197 (Oclacitinib) (APOQUEL?) has recently been approved in the United States and European Union for the control or treatment of pruritus associated with allergic dermatitis and the control or treatment of AD in dogs [1].

Reference:
[1] Gonzales AJ, Bowman JW, Fici GJ, Zhang M, Mann DW, Mitton-Fry M.  Oclacitinib (APOQUEL(?)) is a novel Janus kinase inhibitor with activity against cytokines involved in allergy. J Vet Pharmacol Ther. 2014 Aug;37(4):317-24.
[2] Cosgrove SB, Wren JA, Cleaver DM, Martin DD, Walsh KF, Harfst JA, Follis SL, King VL, Boucher JF, Stegemann MR.  Efficacy and safety of oclacitinib for the control of pruritus and associated skin lesions in dogs with canine allergic dermatitis. Vet Dermatol. 2013 Oct;24(5):479-e114.

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