Product Name

Ruxolitinib (INCB018424)

General description

Ruxolitinib is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities.

Synonym

(3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propanenitrile

Purity

≥98.0%(HPLC)

CAS Number

941678-49-5

Formula

C¹⁷H¹⁸N⁶

Molecular Weight

306.37

Suitability

BioReagent, suitable for cell culture, etc.

l  Physical and Chemical Information

Appearance

solid

Solubility(25℃)

DMSO

≥50mg/mL

Ethanol

≥50mg/mL

Water

Insoluble

l  Biological Information

Biochem/Physiol  Actions

Ruxolitinib is an orally bioavailable Janus-associated kinase (JAK) inhibitor with potential antineoplastic and immunomodulating activities. Ruxolitinib specifically binds to and inhibits  protein tyrosine kinases JAK 1 and 2, which may lead to a reduction in inflammation and an inhibition of cellular proliferation. The JAK-STAT (signal transducer and activator of transcription) pathway plays a key role in the signaling of many cytokines and growth factors and is involved in cellular proliferation, growth, hematopoiesis, and the immune response; JAK kinases may be upregulated in inflammatory diseases, myeloproliferative disorders, and various malignancies.

Ruxolitinib is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM in cell-free assays, >130-fold selectivity for JAK1/2 versus JAK3.

Application

Ruxolitinib is a Janus kinase inhibitor that is used in the treatment of intermediate or high risk myelofibrosis. Ruxolitinib is associated with transient and usually mild elevations in serum aminotransferase during therapy, but has not been ed to cases of clinically apparent idiosyncratic acute liver injury but has been shown to be a cause of reactivation of hepatitis B.

l  Packaging & Storage

Storage temp.

-20℃

l  Precautions and Disclaimer

This product is for R&D use only, not for drug, household, or other uses.

l  References

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov