INCB018424 is an orally bioavailable, potent and selective inhibitor of JAK 1 and JAK2, currently in clinical trials to treat myelofibrosis. In enzyme assays it inhibited JAK1 (IC50=3.2 nM) and JAK2 (4.1 nM), and had selectivity >100 fold for a wide range of other kinases, including JAK3 (428 nM). It acts by blocking the JAK/STAT pathway, and has IC50 of 280nM in cytokine-stimulated whole blood assays.
Technical information:
| Chemical Formula: | C17H18N6 | |
| CAS #: | 941676-49-5 | |
| Molecular Weight: | 306.37 | |
| Purity: | >98% | |
| Appearance: | White solid | |
| Chemical Name: | (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile | |
| Solubility: | Up to 100 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | A Quintas-Cardama et al. Preclinical characterization of the selective JAK1/2 inhibitor INCB018424: therapeutic implications for the treatment of myeloproliferative neoplasms. Blood 2010, 115(15), 3109-3117. |
| 2. | S Verstovsek et al. Safety and efficacy of INCB018424, a JAK1 and JAK2 inhibitor, in myelofibrosis. N. Engl. J. Med. 2010, 363(12), 1117-1127. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
