Biological Activity
Ruxolitinib (INCB018424) is a potent, selective and orally bioavailable inhibitor of JAK1 and JAK2 with IC50 of 2.7 and 4.5 nM, respectively. It shows modest selectivity against Tyk2 (IC50, 19 nM) and marked selectivity against JAK3 (IC50, 322 nM) [1]. INCB018424 inhibits IL-6 signaling (IC50, 281 nM), and proliferation of JAK2V617F+ Ba/F3 cells (IC50, 126 nM) as well as HEL cells (IC50, 186 nM) with JAK2 mutation. INCB018424 preferentially suppresses erythroid progenitor colony formation from JAK2V617F+ PV patients (IC50, 67 nM) versus healthy donors (IC50, >400 nM). In a mouse model of JAK2V617F+ MPN, oral INCB018424 markedly reduces splenomegaly and circulating levels of inflammatory cytokines, and preferentially eliminates neoplastic cells, resulting in significantly prolonged survival without myelosuppressive or immunosuppressive effects. The preclinical results support its clinical evaluation as a promising oral agent for the treatment of myeloproliferative neoplasms (MPNs), including MF, PV, and ET [2-3]. INCB018424 appears safe and well-tolerated dose of 15 mg BID and demonstrates preliminary efficacy in the treatment of Rheumatoid arthritis (RA) [4].
Chemical Properties
| Cas No.: 941678-49-5 | M. Wt.: 306.37 |
| Formula: C17H18N6 | Purity: >99% |
| Synonym: INCB018424, INCB18424, NCB018424, NCB18424 | |
| Chemical Name: (3R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl] propanenitrile | |
| Appearance: White to off-white solid | |
| Solubility: Soluble in DMSO (20 mg/mL) and ethanol (15 mg/mL with warming), sparingly soluble in water | |
| Storage：Store solid at -20 ºC for the stability of two years | |
Application Concentration (Just for reference)
The appropriate working concentration of Ruxolitinib depends on cell types, cell culture properties and specific applications. It is recommended that researchers start with optimal experiments for first use.
