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CEP-33779

In stock
Catalog No.
A4146
JAK2 inhibitor,highly selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$250.00
In stock
5mg
$170.00
In stock
10mg
$230.00
In stock
50mg
$770.00
In stock
100mg
$1,130.00
In stock

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Background

CEP-33779, is a highly selective, orally active inhibitor of Janus kinase 2 (JAK2). When evaluate against the other members of the JAK family, CEP-33779 demonstrates varying degrees of selectivity from >40-fold versus JAK1 to >800-fold against TYK2. In a cellular system, CEP-33779 is shown to inhibit JAK2 in irf-bla TF-1 cells utilizing the GeneBLAzer reporter assay. It is also able to mitigate several immune parameters associated with SLE advancement, including the protection and treatment of mice with lupus nephritis. The ability of CEP-33779 to suppress growth of colorectal tumors by inhibiting the IL-6/JAK2/STAT3 signaling suggests a potential therapeutic utility of JAK2 inhibitors in multiple tumors types, particularly those with a strong inflammatory component.

Reference

Kristine L Stump, Lily D Lu, Pawel Dobrzanski, Cynthia Serdikoff, Diane E Gingrich, Ben J Dugan, Thelma S Angeles, Mark S Albom, Mark A Ator, Bruce D Dorsey, Bruce A Ruggeri, Matthew M Seavey. A highly selective, orally active inhibitor of Janus kinase 2, CEP-33779, ablates disease in two mouse models of rheumatoid arthritis. Arthritis Research & Therapy 2011, 13:R68.

Lily D. Lu, Kristine L. Stump, Nate H. Wallace, Pawel Dobrzanski, Cynthia Serdikoff, Diane E. Gingrich, Benjamin J. Dugan, Thelma S. Angeles, Mark S. Albom, Jennifer L. Mason, Mark A. Ator, Bruce D. Dorsey, Bruce A. Ruggeri, Matthew M. Seavey. Depletion of Autoreactive Plasma Cells and Treatment of Lupus Nephritis in Mice Using CEP-33779, a Novel, Orally Active, Selective Inhibitor of JAK2. The Journal of Immunology October 1, 2011 vol. 187 no. 7 3840-3853.

Matthew M. Seavey, Lily D. Lu, Kristine L. Stump, Nate H. Wallace, William Hockeimer, Teresa M. O'Kane, Bruce A. Ruggeri, Pawel Dobrzanski. Therapeutic Efficacy of CEP-33779, a Novel Selective JAK2 Inhibitor, in a Mouse Model of Colitis-Induced Colorectal Cancer. Mol Cancer Ther April 2012 11; 984.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt462.57
Cas No.1257704-57-6
FormulaC24H26N6O2S
SynonymsCEP 33779,CEP33779
Solubility≥23.15 mg/mL in DMSO with gentle warming, <1.98 mg/mL in EtOH
Chemical NameN-[3-(4-methylpiperazin-1-yl)phenyl]-8-(4-methylsulfonylphenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine
SDFDownload SDF
Canonical SMILESCN1CCN(CC1)C2=CC(=CC=C2)NC3=NN4C=CC=C(C4=N3)C5=CC=C(C=C5)S(=O)(=O)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description CEP-33779 is a selective inhibitor of JAK2 with IC50 value of 1.8 nM.
Targets JAK2          
IC50 1.8 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

CEP-33779

Related Biological Data

CEP-33779