2. Epigenetics Stem Cell/Wnt Protein Tyrosine Kinase/RTK JAK/STAT Signaling
  3. JAK
  4. Oclacitinib

Oclacitinib  (Synonyms: PF-03394197)

Cat. No.: HY-13577 Purity: 99.23%
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Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).

For research use only. We do not sell to patients.

Oclacitinib Chemical Structure

Oclacitinib Chemical Structure

CAS No. : 1208319-26-9

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of Oclacitinib:

Oclacitinib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Oclacitinib

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  • Biological Activity

  • Protocol

  • Purity & Documentation

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Description

Oclacitinib is a novel JAK inhibitor. Oclacitinib is most potent at inhibiting JAK1 (IC50=10 nM).

IC50 & Target

JAK1

10 nM (IC50)

JAK2

18 nM (IC50)

Tyk2

84 nM (IC50)

JAK3

99 nM (IC50)

In Vitro

Using isolated enzyme systems and in vitro human or canine cell models, potency and selectivity of Oclacitinib is determined against JAK family members and cytokines that trigger JAK activation in cells. Inhibitory activity of Oclacitinib against JAK family members is determined in isolated enzyme systems. Oclacitinib inhibits JAK1, JAK2, JAK3, and TYK2 by 50% at concentrations (IC50's) of 10, 18, 99, and 84 nM, respectively. Oclacitinib is most potent against the JAK1 enzyme, showing a 1.8-fold selectivity for JAK1 vs. JAK2 and 9.9-fold selectivity toward JAK1 vs. JAK3. Oclacitinib inhibits JAK family members by 50% at concentrations (IC50's) ranging from 10 to 99 nM and does not inhibit a panel of 38 non-JAK kinases (IC50's > 1000 nM). Oclacitinib also inhibits the function of JAK1-dependent cytokines involved in allergy and inflammation (IL-2, IL-4, IL-6, and IL-13) as well as pruritus (IL-31) at IC50's ranging from 36 to 249 nM. Oclacitinib has minimal effects on cytokines that does not activate the JAK1 enzyme in cells (erythropoietin, granulocyte/macrophage colony-stimulating factor, IL-12, IL-23; IC50's > 1000 nM) [1].Topical treatment with Tofacitinib (0.1%) and Oclacitinib (0.1%) leads to significant reduction of cell migration from mouse ear explants compared with vehicle-treated ears (all P < 0.05). The cell counts of MHC class II positive cells (that is, Langerhans cells) are significantly lower in vehicle-treated compared with each JAK inhibitor–treated epidermis (all P < 0.01) [2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Oclacitinib Related Antibodies
In Vivo

Scratching bouts at the high dose in the Oclacitinib group are significantly less than in the vehicle-only group (P<0.01)[2]. Client-owned dogs (n=436) with moderate to severe owner-assessed pruritus and a presumptive diagnosis of allergic dermatitis are enrolled. Dogs are randomized to either Oclacitinib at 0.4-0.6 mg/kg orally twice daily or an excipient-matched placebo. An enhanced 10 cm visual analog scale (VAS) is used to assess the severity of pruritus from day 0 to 7 and to assess the severity of dermatitis on days 0 and 7. Dogs can remain on the study for 28 days. Oclacitinib produces a rapid onset of efficacy within 24 h[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

337.44

Formula

C15H23N5O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN([C@H]1CC[C@@H](CC1)CS(NC)(=O)=O)C2=C3C(NC=C3)=NC=N2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 44 mg/mL (130.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9635 mL 14.8174 mL 29.6349 mL
5 mM 0.5927 mL 2.9635 mL 5.9270 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.23%

COA (254 KB) LCMS (258 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Recombinant human active kinase domains for JAK1, JAK2, JAK3, and TYK2 are used in isolated enzyme assays using Caliper microfluidics technology to determine potency of Oclacitinib against the JAK family members. Sequence homology to the analogous sequences in the canine JAK enzymes are 98, 98, 100, and 90%, respectively. Invitrogen kinase panel testing is performed to determine potency of Oclacitinib toward 38 different non-JAK kinases using their SelectScreen Kinase Profiling Services. Oclacitinib is evaluated at a concentration of 1 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2][3]

Mice[2]
BALB/cAnN (female, 6 weeks old) are used. The JAK inhibitors (Tofacitinib or Oclacitinib) are administered orally or topically 30 minutes before and 4 hours after toluene-2,4-diisocyanate (TDI) challenge because the absorption of Tofacitinib and Oclacitinib is rapid, with plasma concentrations for both Tofacitinib and Oclacitinib peaking at around 1 hour after oral or intravenous administration. Tofacitinib and Oclacitinib both have a short half-life of 2 and 4 hours after administration, respectively. Each drug is diluted in a 0.5% methylcellulose/0.25% Tween 20 solution for oral administration, and a 7:1 acetone:DMSO solution for topical application to concentrations described subsequently. For each drug, a vehicle-only control group and low- and high-dose groups are set. Oral doses are as follows: Tofacitinib, 10 and 30 mg/kg; and Oclacitinib, 30 and 45 mg/kg. Topically administered doses are 0.1, 0.25, and 0.5% for both chemicals. The oral doses of Tofacitinib and Oclacitinib used in this study are selected.
Dogs[3]
Dogs are randomized to one of two treatment groups (i.e. Oclacitinib or placebo) in a 1:1 ratio. Dogs in the Oclacitinib treatment group are given Oclacitinib maleate caplets orally at a dose of 0.4-0.6 mg/kg twice daily. The scored caplets are provided in three strengths containing 3.6, 5.4 and 16 mg of Oclacitinib. Dogs in the placebo treatment group are given the same number of caplets, identical in appearance to Oclacitinib maleate caplets and containing all of the same excipients except Oclacitinib maleate.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9635 mL 14.8174 mL 29.6349 mL 74.0872 mL
5 mM 0.5927 mL 2.9635 mL 5.9270 mL 14.8174 mL
10 mM 0.2963 mL 1.4817 mL 2.9635 mL 7.4087 mL
15 mM 0.1976 mL 0.9878 mL 1.9757 mL 4.9391 mL
20 mM 0.1482 mL 0.7409 mL 1.4817 mL 3.7044 mL
25 mM 0.1185 mL 0.5927 mL 1.1854 mL 2.9635 mL
30 mM 0.0988 mL 0.4939 mL 0.9878 mL 2.4696 mL
40 mM 0.0741 mL 0.3704 mL 0.7409 mL 1.8522 mL
50 mM 0.0593 mL 0.2963 mL 0.5927 mL 1.4817 mL
60 mM 0.0494 mL 0.2470 mL 0.4939 mL 1.2348 mL
80 mM 0.0370 mL 0.1852 mL 0.3704 mL 0.9261 mL
100 mM 0.0296 mL 0.1482 mL 0.2963 mL 0.7409 mL
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Oclacitinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Oclacitinib1208319-26-9PF-03394197PF03394197PF 03394197JAKJanus kinaseInhibitorinhibitorinhibit

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