Uses
(3S)-3-Cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile is a newly developed JAK2 inhibitor therapy aimed to improve MPN-associated splenomegaly and systemic symptoms. The opposite enantiomer of Ruxolitinib (R702000).
Biological Activity
s-ruxolitinib is the chirality of incb018424, is a potent and selective small-molecule janus kinase 1 (jak1) and jak2 inhibitor. it was initially developed to target the constitutive activation of the jak-stat pathway. janus kinases (jaks) are a family of cytoplasmic tyrosine kinases that mediates signals from the receptors for various cytokines and growth factors that have a key role in haematopoiesis and immune function. ruxolitinib maintains its anti-jak activity by competitive inhibition of the atp-binding catalytic site of the kinase domain. ruxolitinib is well absorbed at >95%. exposure of jak2v617f-positive ba/f3 cells to ruxolitinib iss shown to result in reduced cellular proliferation.ruben a. mesa, uma yasothan, peter kirkpatrick. ruxolitinib. nature reviews drug discovery. 2012; 11: 103-104john mascarenhas, ronald hoffman. ruxolitinib: the first fda approved therapy for the treatment of myelofibrosis. clinical cancer research. 2012; 18(11): 3008 - 3014
