Ilginatinib maleate 是一种可口服的JAK2强效抑制剂，IC50值为 0.72 nM，对其选择性是对 JAK1、JAK3和 Tyk2 的 46、54 和 22 倍，IC50分别为 33、39 和 22 nM。

Ilginatinib maleate is a highly active and orally bioavailable inhibitor of JAK2.

Ilginatinib maleate(NS-018 maleate) is highly active against JAK2 with a 50% inhibition (IC(50)) of<1 n, and had 30-50-fold greater selectivity for JAK2 over other JAK-family kinases, such as JAK1, JAK3 and tyrosine kinase 2.?In addition to JAK2, NS-018 inhibited Src-family kinases.?NS-018 showed potent antiproliferative activity against cell lines expressing a constitutively activated JAK2 (the JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene;?IC(50)=11-120 n), but showed only minimal cytotoxicity against most other hematopoietic cell lines without a constitutively activated JAK2[1].

Ilginatinib maleate(NS-018 maleate) preferentially suppressed in vitro erythropoietin-independent endogenous colony formation from polycythemia vera patients.?NS-018 also markedly reduced splenomegaly and prolonged the survival of mice inoculated with Ba/F3 cells harboring JAK2V617F.?In addition, NS-018 significantly reduced leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improved nutritional status, and prolonged survival in JAK2V617F transgenic mice.?suggest that NS-018 will be a promising candidate for the treatment of MPNs[1].

1354799-87-3

C25H24FN7O4

505.5

NS-018 maleate

H2O:< 0.1 mg/mL (insoluble)
DMSO:30 mg/mL (59.35 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years