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CEP-33779

Cat. No. M2064
CEP-33779 Structure
Synonym:

CEP33779

Size Price Availability
10mg USD 340 Out of stock
50mg USD 1080 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

CEP-33779 is a highly selective, orally active, small-molecule inhibitor of JAK2. CEP-33779 (< 3 μM) inhibits phosphorylation of downstream target signal transducer and activator of transcription 5 (pSTAT5) of JAK2 in a concentration dependent manner in HEL92 cells. CEP-33779 induced regression of established colorectal tumors, reduced angiogenesis, and reduced proliferation of tumor cells. CEP-33779 results in reduced bone degradation, reduced tissue destruction, and reduced osteoarthritis in dose-dependent manner in CAIA or CIA mice. CEP-33779 suppressed growth of colorectal tumors by inhibiting the IL-6/JAK2/STAT3 signaling. Treatment with CEP-33779 extended survival and reduced splenomegaly/lymphomegaly. Several serum cytokines were significantly decreased upon treatment including IL-12, IL-17A, IFN-α, IL-1β, and TNF-α.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 462.57
Formula C24H26N6O2S
CAS Number 1257704-57-6
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

Therapeutic efficacy of CEP-33779, a novel selective JAK2 inhibitor, in a mouse model of colitis-induced colorectal cancer.
Seavey MM, et al. Mol Cancer Ther. 2012 Apr;11(4):984-93. PMID: 22334590.

Depletion of autoreactive plasma cells and treatment of lupus nephritis in mice using CEP-33779, a novel, orally active, selective inhibitor of JAK2.
Lu LD, et al. J Immunol. 2011 Oct 1;187(7):3840-53. PMID: 21880982.

A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis.
Stump KL, et al. Arthritis Res Ther. 2011 Apr 21;13(2):R68. PMID: 21510883.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CEP-33779, CEP33779 supplier, JAK, inhibitors

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