JAK1/2 inhibitor,potent and selective
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Description||S-Ruxolitinib is the chirality of INCB018424.|
|IC50||3.3 nM||2.8 nM||428 nM|
|Cas No.||941685-37-6||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at -20°C|
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: 103-104
John Mascarenhas, Ronald Hoffman. Ruxolitinib: The First FDA Approved Therapy for the Treatment of Myeloﬁbrosis. Clinical Cancer Research. 2012; 18(11): 3008 - 3014