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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. PMC8472008
U937 cells 10 µM 72 hours Evaluate the effect of TCP combined with ATRA on the differentiation of U937 cells, results showed that the combination treatment significantly increased CD11b expression. PMC10989010
K7M2 cells 1 μM 72 hours Evaluate the effect of Oclacitinib on osteosarcoma cell proliferation, showing no significant inhibitory effect at 1 μM PMC8540451
MG63.3 cells 1 μM 72 hours Evaluate the effect of Oclacitinib on osteosarcoma cell proliferation, showing no significant inhibitory effect at 1 μM PMC8540451
CD8+ T cells 10^-6 M and 10^-7 M 72 hours Study of abacavir-induced immunotoxicity PMC8472008
CD4+ T cells 10^-6 M and 10^-7 M 72 hours Inhibited Th17 cell differentiation by modulating protein acetylation PMC8472008

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Shiba Inu dogs Canine atopic dermatitis model Oral 2 weeks or an average of 13.24 months To evaluate the therapeutic effect of oclacitinib on canine atopic dermatitis and its impact on skin and gut microbiota. Results showed that oclacitinib treatment significantly reduced the abundance of Staphylococcus on the skin and altered the gut microbiota composition, bringing it closer to that of healthy dogs. PMC10590023
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. PMC10989010
Dogs Spontaneous high-grade soft tissue sarcoma Oral Twice daily for 14 days Evaluate the effect of oclacitinib combined with MYXV ΔSERP2 therapy on canine soft tissue sarcoma. Results showed no significant improvement in tumor regrowth time. PMC10525839
Dogs Canine atopic dermatitis model Oral 4 and 8 weeks To evaluate the therapeutic effect of oclacitinib on canine atopic dermatitis, results showed significant improvement in skin condition. PMC8541266

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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