1354799-87-3

Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

Ilginatinib maleate (NS-018 maleate) is a highly potent, orally available JAK2 inhibitor with IC50 of 0.72 nM, 46-fold selectivity for JAK1 (IC50, 33 nM) and 54-fold for JAK3 ( IC50, 39 nM), and 22 times that of Tyk2 (IC50, 22 nM).

Ilginatinib maleate (NS-018 maleate) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model.

JAK2 0.72 nM (IC 50 )

Tyk2 22 nM (IC 50 )

JAK1 33 nM (IC 50 )

JAK3 39 nM ( IC 50 )

JAK2: 0.72 nM (IC₅₀); Tyk2: 22 nM (IC₅₀); JAK1: 33 nM (IC₅₀); JAK3: 39 nM (IC₅₀)

Store at -20°C

[1] 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;1(7):e29. DOI:10.1038/bcj.2011.29
[2] 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. DOI:10.1016/j.leukres.2014.03.001