Oclacitinib maleate

SKU: orb1300351

Description

Oclacitinib maleate is a selective Janus kinase (JAK) inhibitor with IC50 values of 10-99 nM against JAK family members. It potently inhibits JAK1-dependent cytokine signaling and demonstrates high selectivity over other kinases. This compound is widely used in preclinical research for investigating allergic dermatitis and pruritus in both in vitro and in vivo models.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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Key Properties

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CAS Number	1640292-55-2
MW	453.51
Purity	99.92% (May vary between batches)
Formula	C₁₅H₂₃N₅O₂S·C₄H₄O₄
SMILES	OC(=O)\C=C\C(O)=O.CNS(=O)(=O)C[C@H]1CC[C@@H](CC1)N(C)c1ncnc2[nH]ccc12
Target	JAK,Tyrosine Kinases
Solubility	10% DMSO+40% PEG300+5% Tween-80+45% Saline:3.3 mg/mL (7.28 mM);Ethanol:83 mg/mL (183.02 mM);H2O:15 mg/mL (33.08 mM);DMSO:83 mg/mL (183.02 mM)

Bioactivity

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Target IC50	JAK1-dependent:36 to 249 nM\|JAK:10 to 99 nM
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. Read more...
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. Read more...

Storage & Handling

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Storage	keep away from direct sunlight,keep away from moisture,store under nitrogen \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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inhibit, Janus kinase, JAK, JAK1, JAK1-dependent, JAK2, JAK3, Oclacitinib, Oclacitinib maleate, Oclacitinib Maleate, Inhibitor, Tyrosine Kinases, TyrosineKinases, TYK2, PF 03394197, PF 03394197 Maleate, PF03394197, PF-03394197, PF03394197 Maleate, PF-03394197 maleate, PF-03394197 Maleate

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Compound Identifiers

PubChem CID

56843700 ↗

Key Properties

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No computed properties available.

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