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Chemical Structure| 1257704-57-6 Chemical Structure| 1257704-57-6

Structure of CEP-33779
CAS No.: 1257704-57-6

Chemical Structure| 1257704-57-6

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CEP-33779 is a highly selective JAK2 inhibitor with IC50 value of 1.8 nM, with much less potency against JAK1 and TYK2 with >40- and >800-fold IC50 values.

4.5 *For Research Use Only !

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Product Details of CEP-33779

CAS No. :1257704-57-6
Formula : C24H26N6O2S
M.W : 462.57
SMILES Code : O=S(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(C)=O
MDL No. :MFCD22683932
InChI Key :RFZKSQIFOZZIAQ-UHFFFAOYSA-N
Pubchem ID :57336812

Safety of CEP-33779

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

Related Pathways of CEP-33779

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target
  • JAK2

    JAK2, IC50:1.8 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
MH-S cells 3000 nM 24 h CEP-33779 significantly improved the LPS-induced reduction in phagocytic activity of MH-S cells PMC11628351
KBV20C cells 2 µM 24 h CEP-33779 co-treatment with VIC increased cytotoxicity in KBV20C cells, inducing early apoptosis. PMC9100550
NCI-H1975 1.6, 3.2, 16 µM 48 h To evaluate the cytotoxicity of CEP-33779 in combination with allopurinol on resistant cell lines. The results showed that combination treatment significantly reduced cell viability, indicating a synergistic effect. PMC6670022
HCC827 1.6, 3.2, 16 µM 48 h To evaluate the cytotoxicity of CEP-33779 in combination with allopurinol on resistant cell lines. The results showed that combination treatment significantly reduced cell viability, indicating a synergistic effect. PMC6670022
C3H/HeJ mouse splenocytes 1 μ M 1 h CEP-33779 inhibited JAK2-dependent GM-CSF signaling. PMC8119218
C3H/HeJ mouse HF dermal sheath cells 1 μ M 1 h CEP-33779 inhibited IFN-γ-induced STAT1 tyrosine phosphorylation. PMC8119218

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c mice LPS-induced acute lung injury model Oral 25 mg/kg and 50 mg/kg Twice daily for 48 hours CEP-33779 significantly mitigated LPS-induced lung injury and inflammatory response in mice PMC11628351
Mice Collagen-induced arthritis (CIA) and collagen antibody-induced arthritis (CAIA) models Oral 10 mg/kg, 30 mg/kg, 55 mg/kg, 100 mg/kg Twice daily for 4 to 8 weeks CEP-33779 significantly reduced paw edema and clinical scores in both CIA and CAIA models, and decreased local and serum cytokine levels, indicating its potential for treating rheumatoid arthritis. PMC3132063
NCR-nude mice Tumor xenograft model Oral gavage 10 mg/kg Three times a week for 30 days To evaluate the inhibitory effect of CEP-33779 in combination with allopurinol on tumor growth. The results showed that combination treatment significantly reduced tumor volume, indicating a synergistic effect. PMC6670022
C3H/HeJ mice alopecia areata model systemic administration 50 mg/kg 12 weeks CEP-33779 failed to restore hair regrowth and did not prevent further progressive hair loss. PMC8119218

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.16mL

0.43mL

0.22mL

10.81mL

2.16mL

1.08mL

21.62mL

4.32mL

2.16mL

References

 

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