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Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $33 | In Stock | |
2 mg | $46 | In Stock | |
5 mg | $72 | In Stock | |
10 mg | $101 | In Stock | |
25 mg | $178 | In Stock | |
50 mg | $286 | In Stock | |
100 mg | $480 | In Stock | |
1 mL x 10 mM (in DMSO) | $78 | In Stock |
Description | Oclacitinib maleate (PF-03394197 maleate) is a novel inhibitor of JAK family members, with IC50 values ranging from 10 to 99 nM, and JAK1-dependent cytokines, with IC50 ranging from 36 to 249 nM, while not inhibiting a panel of 38 non-JAK kinases. |
Targets&IC50 | JAK1-dependent:36 to 249 nM, JAK:10 to 99 nM |
In vitro | Oclacitinib inhibits JAK family members by 50% at concentrations ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases. Oclacitinib is most potent at inhibiting JAK1. Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation as well as pruritus. Oclacitinib has minimal effects on cytokines which does not activate the JAK1 enzyme in cells[1]. |
In vivo | Oclacitinib administered orally at a dose of 0.4–0.6 mg/kg twice daily is safe and efficacious in controlling the pruritus associated with allergic dermatitis. Oclacitinib provides itch relief within 24 h that persistes through the treatment period, with over 70% of the treated dogs achieving a >50% reduction in pruritus by day 7[2]. |
Alias | PF-03394197 maleate, PF-03394197 |
Molecular Weight | 453.51 |
Formula | C15H23N5O2S·C4H4O4 |
Cas No. | 1640292-55-2 |
Smiles | OC(=O)\C=C\C(O)=O.CNS(=O)(=O)C[C@H]1CC[C@@H](CC1)N(C)c1ncnc2[nH]ccc12 |
Relative Density. | no data available |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | H2O: 15 mg/mL (33.1 mM) Ethanol: 83 mg/mL (183 mM) DMSO: 83 mg/mL (183 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
H2O/Ethanol/DMSO
Ethanol/DMSO
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