NS-018 maleate

• CAT Number: I001371
• CAS Number: 1354799-87-3
• Molecular Formula: C25H24FN7O4
• Molecular Weight: 505.5
• Purity: ≥95%
• Target: Stem Cell/Wnt
• Solubility: DMSO ≥ 30 mg/mL
• Storage: Store at -20°C

NS-018 maleate is an ATP-competitive small-molecule inhibitor of JAK2 with IC50 of 470nM in Ba/F3-JAK2V617F cells . have30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2.target: JAK2IC 50: 470 nMIn vitro: NS-018 suppressed the phosphorylation of STAT3 in colony-forming cells. NS-018 inhibited Src-family kinases. NS-018 showed potent antiproliferative activity against cell lines expressing a constitutively activated JAK2. NS-018 also markedly reduced splenomegaly and prolonged the survival of mice inoculated with Ba/F3 cells harboring JAK2V617F.In vivo: NS-018 significantly reduced leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improved nutritional status, and prolonged survival in JAK2V617F transgenic mice. NS-018 also inhibited erythroid colony formation in JAK2V617F transgenic mice at significantly lower concentrations than in WT mice.

Reference

[1]. Kuroda J et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

[2]. Nakaya Y et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J, 2011 Jul

[3]. Nakaya Y et al. Effect of NS-018, a selective JAK2V617F inhibitor, in a murine model of myelofibrosis. Blood Cancer J. 2014 Jan 10