S-Ruxolitinib (INCB018424)
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.
References
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
| Storage | Store at -20°C |
| M.Wt | 306.37 |
| Cas No. | 941685-37-6 |
| Formula | C17H18N6 |
| Solubility | Soluble in DMSO |
| Chemical Name | (3S)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile |
| SDF | Download SDF |
| Canonical SMILES | C1CCC(C1)C(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Description | S-Ruxolitinib is the chirality of INCB018424. | |||||
| Targets | JAK1 | JAK2 | JAK3 | |||
| IC50 | 3.3 nM | 2.8 nM | 428 nM | |||
Quality Control & MSDS
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Chemical structure
