Ilginatinib hydrochloride

Ilginatinib hydrochloride (NS-018 hydrochloride) 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

[1239358-85-0]

Product Name Alternative

NS-018 hydrochloride

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-hydrochloride.html

Purity

98.92

Solubility

DMSO : ≥ 35 mg/mL|H2O : 2 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C21H21ClFN7

Molecular Weight

425.89

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.