A potent, orally available inhibitor of JAK2
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CEP-33779

Item No. 16732

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-(4-methyl-1-piperazinyl)phenyl]-8-[4-(methylsulfonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-amine
CAS Number
1257704-57-6
Molecular Formula
C24H26N6O2S
Formula Weight
462.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mg/ml
SMILES
CS(C1=CC=C(C2=CC=CN3C2=NC(NC4=CC=CC(N5CCN(C)CC5)=C4)=N3)C=C1)(=O)=O
InChi Code
InChI=1S/C24H26N6O2S/c1-28-13-15-29(16-14-28)20-6-3-5-19(17-20)25-24-26-23-22(7-4-12-30(23)27-24)18-8-10-21(11-9-18)33(2,31)32/h3-12,17H,13-16H2,1-2H3,(H,25,27)
InChi Key
RFZKSQIFOZZIAQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $75

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    1 mg

    $120

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    5 mg

    $310

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    Product Description

    CEP-33779 is a potent, orally available inhibitor of JAK2 (IC50 = 1.3 nM).1 It shows 65-fold selectivity for JAK2 over JAK3.1 In mouse models of systemic lupus erythematosus, CEP-33779 reduces the production of inflammatory cytokines, decreases splenomegaly and lymphomegaly, and extends survival.1 It also diminishes inflammatory signaling and improves clinical scores in mice during collagen antibody-induced arthritis and collagen type II-induced arthritis.2 CEP-33779 induces regression of established colorectal tumors in mice, reducing angiogenesis and proliferation of tumor cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lu, L.D., Stump, K.L., Wallace, N.H., et al. Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2. J. Immunol. 187(7), 3840-3853 (2011).

    2. Stump, K.L., Lu, L.D., Dobrzanski, P., et al. A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Arthritis Res. Ther. 13(2), 1-15 (2011).

    3. Seavey, M.M., Lu, L.D., Stump, K.L., et al. Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer. Mol. Cancer Ther. 11(4), 984-993 (2012).