Ruxolitinib (INCB018424) , ≥98% , 941678-49-5

CAS NO.：941678-49-5

Empirical Formula: C17H18N6

Molecular Weight: 306.37

MDL number: MFCD12031592

EINECS: 1312995-182-4

PRODUCT Properties

• Melting point: 84-89°C
• Density: 1.40
• storage temp.: -20°
• solubility: Soluble in DMSO (up to 28 mg/ml) or in Ethanol (up to 15 mg/ml with warming).
• form: White powder.
• pka: 11.63±0.50(Predicted)
• color: White
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.
• InChI: InChI=1/C17H18N6/c18-7-5-15(12-3-1-2-4-12)23-10-13(9-22-23)16-14-6-8-19-17(14)21-11-20-16/h6,8-12,15H,1-5H2,(H,19,20,21)/t15-/s3
• InChIKey: HFNKQEVNSGCOJV-UJHUVDBMNA-N
• SMILES: [C@@H](C1CCCC1)(N1N=CC(C2N=CN=C3NC=CC=23)=C1)CC#N |&1:0,r|

Description and Uses

In November 2011, the U.S. FDA approved ruxolitinib (INCB018424) for the treatment of patients with intermediate or high-risk myelofibrosis. Ruxolitinib is an ATP-competitive inhibitor of JAK1 and JAK2 (IC_50's of 3.3±1.2 nM and 2.8±1.2 nM, respectively) and inhibition occurs regardless of the JAK2V617F mutational status. Ruxolitinib is a moderately potent inhibitor of the related JAK, TYK2 (IC₅₀=19±3.2 nM) but is selective versus JAK3 (IC₅₀=428±243 nM). It was also selective versus a panel of 26 other kinases at concentrations approximately 100-fold the IC₅₀ of JAK1 and JAK2. Inhibition of JAK1 and JAK2 downregulates the JAK-signal transducer and activator of transcription (STAT) pathway, inhibiting myeloproliferation, inducing apoptosis, and reducing numerous cytokine plasma levels.

INCB018424 is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3. Phase 3

Safety

• Symbol(GHS): GHS07,GHS08
• Signal word: Danger
• Hazard statements: H302-H360FD
• Precautionary statements: P202-P280
• HS Code: 29335990