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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.

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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
C3H/HeJ mouse splenocytes 1 μ M 1 h CEP-33779 inhibited JAK2-dependent GM-CSF signaling. JCI Insight. 2021 Apr 8;6(7):e142205.
MH-S cells 3000 nM 24 h CEP-33779 significantly improved the LPS-induced reduction in phagocytic activity of MH-S cells Front Immunol. 2024 Nov 26;15:1472425.
KBV20C cells 2 µM 24 h CEP-33779 co-treatment with VIC increased cytotoxicity in KBV20C cells, inducing early apoptosis. Int J Mol Sci. 2022 Apr 21;23(9):4597.
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. Mol Oncol. 2019 Aug;13(8):1725-1743.
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. Mol Oncol. 2019 Aug;13(8):1725-1743.
C3H/HeJ mouse HF dermal sheath cells 1 μ M 1 h CEP-33779 inhibited IFN-γ-induced STAT1 tyrosine phosphorylation. JCI Insight. 2021 Apr 8;6(7):e142205.

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 Front Immunol. 2024 Nov 26;15:1472425.
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. Arthritis Res Ther. 2011 Apr 21;13(2):R68
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. Mol Oncol. 2019 Aug;13(8):1725-1743.
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. JCI Insight. 2021 Apr 8;6(7):e142205.

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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