NS-018

Product NameNS-018
CAS1239358-86-1
MFC21H20FN7
MW389.43
EINECS
MOL File1239358-86-1.mol

Chemical Properties

Boiling point	574.1±50.0 °C(Predicted)
Density	1.31±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : ≥ 34 mg/mL (87.31 mM)
form	Solid
pka	2.43±0.10(Predicted)
color	Light yellow to yellow

Usage And Synthesis

Uses

Ilginatinib (NS-018) 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).

in vivo

Ilginatinib (NS-018) (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^[1].
Ilginatinib (NS-018) (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice

IC 50

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

References

[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