Ruxolitinib phosphate

• CAT Number: I008849
• CAS Number: 1092939-17-7
• Molecular Formula: C17H21N6O4P
• Molecular Weight: 404.36
• Purity: ≥95%
• Target: JAK
• Solubility: Soluble in DMSO, not in water
• Storage: Store at -20°C
• Related CAS: 941678-49-5(free base)
• IC50: 3.3 nM/2.8 nM(JAK1/JAK2)
• InChI: InChI=1S/C17H18N6.H3O4P/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;1-5(2,3)4/h6,8-12,15H,1-5H2,(H,19,20,21);(H3,1,2,3,4)/t15-;/m1./s1
• InChIKey: JFMWPOCYMYGEDM-XFULWGLBSA-N
• SMILES: N#CC[C@@H](N1N=CC(C2=C3C(NC=C3)=NC=N2)=C1)C4CCCC4.O=P(O)(O)O

Ruxolitinib phosphate (CAT: I008849) is a selective Janus kinase (JAK) inhibitor that has been approved for the treatment of myelofibrosis and polycythemia vera. By inhibiting JAK1 and JAK2, ruxolitinib phosphate suppresses the activity of the JAK-STAT signaling pathway, which plays a crucial role in the pathogenesis of these hematological malignancies. This results in a reduction in splenomegaly, alleviation of disease-related symptoms, and improvement in overall survival. Ruxolitinib phosphate has demonstrated efficacy in clinical trials and is considered a targeted therapy option for patients with myelofibrosis and polycythemia vera.

Reference

1:Pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in renal and hepatic impairment patients. Chen X, Shi JG, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, Punwani NG, Williams WV, Yeleswaram S.Clin Pharmacol Drug Dev. 2014 Jan;3(1):34-42. doi: 10.1002/cpdd.77. Epub 2013 Oct 19. PMID: 27128228
2:Population pharmacokinetic analysis of orally-administered ruxolitinib (INCB018424 Phosphate) in patients with primary myelofibrosis (PMF), post-polycythemia vera myelofibrosis (PPV-MF) or post-essential thrombocythemia myelofibrosis (PET MF). Chen X, Williams WV, Sandor V, Yeleswaram S.J Clin Pharmacol. 2013 Jul;53(7):721-30. doi: 10.1002/jcph.102. Epub 2013 May 16. PMID: 23677817
3:The effect of CYP3A4 inhibition or induction on the pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in healthy volunteers. Shi JG, Chen X, Emm T, Scherle PA, McGee RF, Lo Y, Landman RR, McKeever EG Jr, Punwani NG, Williams WV, Yeleswaram S.J Clin Pharmacol. 2012 Jun;52(6):809-18. doi: 10.1177/0091270011405663. Epub 2011 May 20. PMID: 21602517
4:The pharmacokinetics, pharmacodynamics, and safety of orally dosed INCB018424 phosphate in healthy volunteers. Shi JG, Chen X, McGee RF, Landman RR, Emm T, Lo Y, Scherle PA, Punwani NG, Williams WV, Yeleswaram S.J Clin Pharmacol. 2011 Dec;51(12):1644-54. doi: 10.1177/0091270010389469. Epub 2011 Jan 21. PMID: 21257798