A4149-1mg | S-Ruxolitinib (INCB018424) [941685-37-6] Clinisciences

Background

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

Chemical Properties

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.

Biological Activity

Description	S-Ruxolitinib is the chirality of INCB018424.
Targets	JAK1	JAK2	JAK3
IC50	3.3 nM	2.8 nM	428 nM

Quality Control

Purity = 99.34%

S-Ruxolitinib (INCB018424) [941685-37-6]

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Background

Chemical Properties

Biological Activity

Quality Control