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Biological Activity:
An orally bioavailable, potent and selective inhibitor of Janus-associated kinase (JAK) 1 and 2, with IC50 to be 2.7, 4.5 and 332 nM for JAK1, JAK2 and JAK3 respectively; selectivity >100 fold for a wide range of other kinases. It acts by blocking the JAK/STAT pathway.
References:
RA Mesa. Ruxolitinib, a selective JAK1 and JAK2 inhibitor for the treatment of myeloproliferative neoplasms and psoriasis. IDrugs. 2010, 13(6), 394-403. [online]
C Campas-Moya. Ruxolitinib. Drugs Fut. 2010, 35(6), 457. [online]
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.
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.
E Apostolidou et al. JAK2 inhibitors: a reality? a hope? Clin. Lymp Myel. 2009, 9(Suppl. 3), S340-S345.
Q Lin et al. Enantioselective synthesis of Janus kinase inhibitor INCB018424 via an organocatalytic aza-Michael reaction. Org. Lett. 2009, 11(9), 1999-2002.
Chemical Name: (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate
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