Ilginatinib (maleate)

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) .

Product Specifications

CAS Number

[1354799-87-3]

Product Name Alternative

NS-018 (maleate)

UNSPSC

12352005

Target

JAK

Type

Reference compound

Related Pathways

Epigenetics; JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/NS-018-maleate.html

Purity

99.87

Solubility

DMSO : ≥ 30 mg/mL|H2O : < 0.1 mg/mL

Smiles

CN1N=CC(C2=CC(N[C@H](C3=CC=C(F)C=C3)C)=NC(NC4=NC=CN=C4)=C2)=C1.O=C(O)/C=C\C(O)=O

Molecular Formula

C25H24FN7O4

Molecular Weight

505.50

References & Citations

[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.|[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.