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Chemical Structure| 1640292-55-2 Chemical Structure| 1640292-55-2

Structure of Oclacitinib maleate
CAS No.: 1640292-55-2

Chemical Structure| 1640292-55-2

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Oclacitinib Fumarate is a potent JAK inhibitor with IC50 value ranging in 10-99 nM for JAK family members, most potent against JAK1 with IC50 value of 10 nM.

Synonyms: PF-03394197 maleate; PF-03394197; Oclacitinib maleate

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Product Details of Oclacitinib maleate

CAS No. :1640292-55-2
Formula : C19H27N5O6S
M.W : 453.51
SMILES Code : O=S(C[C@H]1CC[C@H](N(C)C2=C3C(NC=C3)=NC=N2)CC1)(NC)=O.O=C(O)/C=C/C(O)=O
Synonyms :
PF-03394197 maleate; PF-03394197; Oclacitinib maleate
MDL No. :MFCD30533388
InChI Key :VQIGDTLRBSNOBV-BTJKTKAUSA-N
Pubchem ID :44631937

Safety of Oclacitinib maleate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of Oclacitinib maleate

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK1

    JAK1, IC50:10nM

  • JAK3

    JAK3, IC50:99nM

  • Tyk2

    TYK2, IC50:84nM

  • JAK2

    JAK2, IC50:18nM

In Vitro:

Cell Line
Concentration Treated Time Description References
CD49b+CD223+CD4+ T cells 10^-6 M and 10^-7 M 72 hours To evaluate the effect of OCL on Tr1 cells (CD49b+CD223+CD4+ T cells). Results showed that OCL significantly reduced the percentage and absolute count of Tr1 cells. Molecules. 2021 Sep 17;26(18):5655.
CD8+ T cells 10^-6 M and 10^-7 M 72 hours To evaluate the effect of OCL on IL-4, IFN-γ, and IL-17 production in CD8+ T cells. Results showed that OCL significantly reduced the percentage and absolute count of IL-4+IFN-γ- CD8+ T cells but had no significant effect on IFN-γ and IL-17 production. Molecules. 2021 Sep 17;26(18):5655.
CD4+ T cells 10^-6 M and 10^-7 M 72 hours To evaluate the effect of OCL on IL-4, IFN-γ, and IL-17 production in CD4+ T cells. Results showed that OCL reduced the percentage of IL-4+IFN-γ- CD4+ T cells but had no significant effect on IFN-γ and IL-17 production. Molecules. 2021 Sep 17;26(18):5655.
U937 cells 10 µM 72 hours To screen JAK inhibitors with anti-inflammatory activity, inhibiting influenza virus-induced pro-inflammatory cytokines (IP-10, MCP-1, IL-8) production. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0135023.
K7M2 cells 10 pM-100 μM 72 hours Evaluate the effect of Oclacitinib on osteosarcoma cell proliferation, showing no significant inhibitory effect at 1 μM Pharmaceuticals (Basel). 2021 Sep 25;14(10):971.
MG63.3 cells 10 pM-100 μM 72 hours Evaluate the effect of Oclacitinib on osteosarcoma cell proliferation, showing no significant inhibitory effect at 1 μM Pharmaceuticals (Basel). 2021 Sep 25;14(10):971.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice Lethal influenza virus infection model Intraperitoneal injection 20 mg/kg/d Twice daily for 5 days To evaluate the therapeutic efficacy of oclacitinib against lethal influenza virus infection, results showed that 20 mg/kg/d significantly improved survival rate (70%), reduced pro-inflammatory cytokine production and lung inflammatory cell infiltration. Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0135023.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.21mL

0.44mL

0.22mL

11.03mL

2.21mL

1.10mL

22.05mL

4.41mL

2.21mL

References

 

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